SlideShare a Scribd company logo
1 of 92
By,
 Dr. Shreeraj Shah
 Associate Professor,
 Dept. of Pharmaceutical
  Technology
 L.J. Institute of Pharmacy,
  Ahmedabad
   Bioadhesion may be defined as the state in which two materials, at least
    one of which is biological in nature, are held together for extended
    periods of time by interfacial forces.
   The rationale being that the formulation will be ‘held’ on a biological
    surface for localized drug delivery.
   The API will be released close to the site of action with a consequent
    enhancement of bioavailability.
   It is a phenomenon of interfacial molecular attractive forces amongst the
    surfaces of the biological substrate and the natural or synthetic polymers,
    which allows the polymer to adhere to the biological surface for an
    extended period of time
   For the purpose of drug delivery system
    Drug carrier system  adhere to biological tissue  increase
    concentration gradient at the absorption site  increase the
    bioavailability.
   Also used for
    • local target to the mucosal surface
    • reduce the side effect
 Mucoadhesion is commonly defined as the
adhesion between two materials, at least one of
which is a mucosal surface.

 Mucoadhesive dosage forms may be
designed to enable prolonged retention at the
site of application, providing a controlled rate of
drug release for improved therapeutic outcome.
 Bioadhesion is defined as an ability of a material
to adhere to a biological tissue for an extended
period of time.

 In the case of polymer attached to the mucin
layer of a mucosal tissue, the term “mucoadhesion”
is used.
The ideal characteristics of a Bio/Mucoadhesive
approach include:

The rapid adherence to the mucosal layer without any
 change in the physical property of the delivery matrix,

minimum interference to the release of the active
 agent,

biodegradable     without    producing     any      toxic
byproducts,

 enhance the penetration of the active agent (if the
  active agent is meant to be absorbed from the delivery
  site)
   The formulation stays longer at the delivery site improving API bioavailability using lower API
    concentrations for disease treatment
   The use of specific bioadhesive molecules allows for possible targeting of particular sites or
    tissues
   Increased residence time combined with controlled API release may lead to lower
    administration frequency
   The avoidance of first-pass metabolism
   Dose-related side effects may be reduced due to API localization at the disease site
   These dosage forms facilitate intimate contact of the formulation with the underlying absorption
    surface. This allows modification of tissue permeability for absorption of macromolecules
    ,such as peptides and proteins. Inclusion of penetration enhancers such as Sodium glycocholate,
    Sodium taurocholate and L-lysophosphotidyl choline and protease inhibitors in the
    mucoadhesive dosage forms resulted in better absorption of peptides and proteins.
   Medications administered orally do not enter the blood stream
    immediately after passage through the buccal mucosa. Instead they
    have to be swallowed and then have to pass through a portion of the
    GIT before being absorbed. So the action is not very rapid in the GIT
    as compared when the drug is administered through buccal route.
   Certain drugs when ingested undergo drug destruction, there are
    several drugs which are potentially in this category. Many drugs
    affect liver metabolism and also cause destruction via first pass
    metabolism of other drugs.
   Oral ingestions results in more exposure of a drug to the GI tract.
    One of the side effects of many antibiotics is the destruction of
    normal GI flora resulting in diarrhea and overgrowth with dangerous
    organisms such as C. difficile.
   The absorption of mucoadhesive drugs is adversely affected by the
    presence of food. Tetracyclines, in particular, complicates the
    administration of this class of antibiotics via the oral route.
   Mucoadhesive Inner layers called mucosa Inner
    epithelial Cell lining Covered with viscoelastic
    fluid.
   It is secreted by Goblet cells lining the epithelia or
    by special exocrine glands with mucus cells
    composed of water and mucin (an anionic
    polyelectrolyte).
      Other components include proteins, lipids,
    electrolytes and mucopolysaccharides
   Thickness varies from ≈40–50 μm to ≈300 μm
Regions in mucus layer
    General composition of mucus :
     Water……………………….95%
     Glycoprotiens and lipids….0.5-5%
     Mineral salts……………….1%
     Free proteins………………0.5-1%

   These units contain an average of about            8-10
    monosaccharide residues of five different types.
     They are:
     a) L-fucose
     b) D-galactose
     c) N-acetyl-D-glucosamine
     d) N-acetyl-D-galactosamine
     e) Sialic acid
   Complex-high molecular weight macromolecule consisting
    of a polypeptide (protein) backbone to which carbohydrate
    side chains are attached.




                  Generic structure of mucin monomer
Mucus forms flexible, threadlike strands that are internally
cross linked by disulphide bond.




               Disulphide bond present in mucus


The mucus layer which covers the epithelial surface has
various roles:
• Protective
• Barrier
• Adhesion
• Lubrication
MUCUS MEMBRANE STRUCTURE   STRUCTURE OF MUCIN
   The mechanisms responsible in the formation of
    mucoadhesive bonds are not fully known, however
    most research has described mucoadhesive bond
    formation as a three step process.
    Step 1 : Wetting and swelling of polymer (the
             contact stage)
    Step 2 : Interpenetration between the polymer
             chains and the mucosal membrane
    Step 3 : Formation of chemical bonds between the
            entangled chains (both known as
            consolidation stage)
Step 1
 The wetting and swelling step occurs when the polymer
 spreads over the surface of the biological substrate or
 mucosal membrane in order to develop an intimate contact
 with the substrate. This can be readily achieved for
 example by placing a mucoadhesive formulation such as a
 tablet or paste within the oral cavity or vagina. Swelling of
 polymers occur because the components within the
 polymers have an affinity for water.
Step 2
   The surface of mucosal membranes are composed of high
 molecular weight polymers known as glycoproteins. In step 2 of
 the mucoadhesive bond formation, the mucoadhesive polymer
 chains and the mucosal polymer chains intermingle and entangle
 to form semi permeable adhesive bonds. The strength of these
 bonds depends on the degree of penetration between the two
 polymer groups. In order to form strong adhesive bonds, one
 polymer group must be soluble in the other and both polymer
 types must be of similar chemical structure.
Step 3
 This step involves the formation of weak chemical bonds
 between the entangled polymer chains. The types of bonding
 formed between the chains include primary bonds such as
 covalent bonds and weaker secondary interactions such as van
 der Waals Interactions and hydrogen bonds. Both primary and
 secondary bonds are exploited in the manufacture of
 mucoadhesive formulations in which strong adhesions between
 polymers are formed.
 The Theories include :-
(1) The electronic theory.
(2) The wetting theory.
(3) The adsorption theory.
(4) The diffusion theory.
(5)The Fracture theory
(6) The mechanical theory.
(7) The cohesive theory.
 The phenomena of bioadhesion occurs by a complex
  mechanism. There are seven theories have been
  proposed till date
1) The Electronic theory
 Electronic theory is based on the premise that both
  mucoadhesive and biological materials possess opposing
  electrical charges. Thus, when both materials come into
  contact, they transfer electrons leading to the building of a
  double electronic layer at the interface, where the attractive
  forces within this electronic double layer determines the
  mucoadhesive strength
2) The wetting theory
 The wetting theory applies to liquid systems which present
  affinity to the surface in order to spread over it. This
  affinity can be found by using measuring techniques such
  as the contact angle. The general rule states that the lower
  the contact angle then the greater the affinity. The contact
  angle should be equal or close to zero to provide adequate
  spreadability
Bioadhesive drug delivery system
3) The Adsorption theory
 According to the adsorption theory, the mucoadhesive
  device adheres to the mucus by secondary chemical
  interactions, such as in van der Waals and hydrogen
  bonds, electrostatic attraction or hydrophobic
  interactions. For example, hydrogen bonds are the
  prevalent interfacial forces in polymers containing
  carboxyl groups.
 Such forces have been considered the most important
  in the adhesive interaction phenomenon because,
  although they are individually weak, a great number
  of interactions can result in an intense global adhesion
4) The diffusion theory
 Diffusion theory describes the interpenetration of both
  polymer and mucin chains to a sufficient depth to
  create a semi-permanent adhesive bond. It is believed
  that the adhesion force increases with the degree of
  penetration of the polymer chains
 This penetration rate depends on the diffusion
  coefficient, flexibility and nature of the mucoadhesive
  chains, mobility and contact time.
 According      to the literature, the depth of
  interpenetration required to produce an efficient
  bioadhesive bond lies in the range 0.2-0.5 μm
5) The Fracture theory
 This theory attempts to relate the difficulty of
                  separation of two surfaces after adhesion
 It analyzes the force required to separate two surfaces
  after adhesion
  Adhesion Strength = (E ԑ/L )1/2
  E =Young’s modulus of elasticity
  ԑ = Fracture energy
  L = Critical crack length when two surfaces are
       separated
6) The mechanical theory
 Mechanical theory considers adhesion to be due to the
  filling of the irregularities on a rough surface by a
  mucoadhesive liquid. Moreover, such roughness
  increases the interfacial area available to interactions
  thereby aiding dissipating energy and can be
  considered the most important phenomenon of the
  process

7) The cohesive theory
 It proposes that the phenomena of bioadhesion are
  mainly due to the intermolecular interactions amongst
  like-molecules.
   Polymer related factors:
                  Molecular weight
                  Concentration of active polymer
                  Flexibility of polymer chains
                  Hydrogen bonding capacity
                  Presence of functional group
                  Spatial conformation
                  Cross linking density
                  Charge on polymer
                  Hydration
                  Hydrophilicity
   Environment related factors :
                  pH of polymer – substrate interface
                  Applied strength
                  Initial contact time
                  Swelling
   Physiological factors:
                   mucin trun over
POLYMER RELATED FACTORS:-
  1) Molecular weight
 Bioadhesion is maximum at certain molecular weight.
 Low molecular weight  interpenetration is more
 High molecular weight  entanglement is more
 Bioadhesive force of polymers is increase up to molecular
   weight 10000, beyond which there is no further gain.

    2) Concentration of active polymer
    In high concentration coiled molecules of polymer become
     solvent poor and chains available for bioadhesion are less.
    In low concentration bioadhesion of polymer also
     decreases.
3) Degree of hydration
 Depending on the degree of hydration adhesive properties
  are different. It is maximum at a certain degree of hydration.
 High degree of hydration  formation of slippery, non-
  adhesive mucilage due to large amount of water leads to loss
  of adhesiveness.

 4) Charge on polymer
 Mucosal surface is negatively charged. So positively
  charged polymer might facilitate the mucoadhesive process.
 Chitosan have bioadhesion due to electrostatic attraction
  between positively charged D- glucosamine residue of
  chitosan and negatively charged sialic acid residues.
5) Presence of functional group
   Due to immobilization of thiol groups on polymers like chitosan &
    polyacrylic acid their permeation enhancement, enzyme inhibitory &
    mucoadhesive properties are improved.
   The immobilization of thiol groups on microparticles improves
    mucoadhesive properties.
6) Spatial conformation
   Besides molecular weight or chain length, spatial conformation of a polymer
    is also important. Despite a high molecular weight of 19,50,0000 for
    dextrans, they have adhesive strength similar to that of polyethylene glycol
    (PEG), with a molecular weight of 2,00,000. The helical conformation of
    dextran may shield many adhesively active groups, primarily responsible for
    adhesion, unlike PEG polymers, which have a linear conformation.
ENVIRONMENT RELATED FACTORS:-
(1) pH
• pH influences the charge on the surface of both mucus and
   the polymers.
• Mucus will have a different charge density depending on
   the pH because of the difference in the dissociation of the
   functional groups on the carbohydrate moiety and amino
   acids of the polypeptide backbone.
• Polyacrylic acid polymers  degree of hydration increase
   upto pH 4 to 5  slightly increase at pH 6 to 7 
   decreasing at more alkaline pH.
 (2) Applied strength
• To place a solid bioadhesive system, it is necessary to apply
   a defined strength. The adhesion strength increases with the
   applied strength or with the duration of its application, up to
   an optimum level.
(3) Initial contact time
 The initial contact time between the mucoadhesives and the
   mucus layer determines the extent of swelling and the
   interpenetration of the polymer chains.
 The mucoadhesive strength increases as the initial contact
   time increases.

 (4) Swelling
 Interpenetration of chains is easier when polymer chains are
   disentangled and free of interactions.
 When swelling is too great, a decrease in the bioadhesion
   occurs, such phenomena must not occur too early, in order
   to lead to a sufficient time for action of the bioadhesive
   system.
PHYSIOLOGICAL FACTORS:-
(1) Mucin turnover
 The natural turnover of the mucin molecules from the
  mucus layer is important for at least two reasons-
   The mucin turn over is expected to limit the residence
    time of mucoadhesive dosage form on the mucus layer.
   Mucin turnover results in substantial amount of soluble
    mucin molecules. These mucin molecules interact with
    mucoadhesive dosage form before they have a chance to
    interact with the mucus layer.
(2) Disease states
 The physiological properties of the mucus are known to
  change during disease conditions such as the common cold,
  gastric ulcers etc. The exact structural changes taking place
  in mucus under these conditions are not yet clearly
  understood.
 They are water soluble and water insoluble
  polymers which are swellable networks joined by
  cross linking agents.
 Characteristic of ideal polymer
 Degradation products should be non toxic and non
  absorbable from GIT
 Good spreadability, wetting, swelling, solubility
  and biodegradability properties
 Optimum molecular weight
 Non irritant to mucous membrane
 Form a strong non covalent bond with mucin
  epithelial cell surfaces
 Adhere quickly to moist tissue
 Allow easy incorporation of the drug
 Not decompose on storage or during shelf life of dosage
  form
 Should possess site specificity
 Cost effective
 Should approved by regulatory authorities
According to source
Natural and modified natural        Synthetic
Agaros                              Carbopol
Chitosan                            Polycarbophil
Gelatin                             Polyacrylic acid
Hyaluronic acid                     Polyacrylates
Carrageenan                         Methacrylic acid
Pectin                              Poly Vinyl Alcohol
Sodium alginate                     Poly Vinyl Pyrollidine
Carboxy Methyl Cellulose            Ethylhexaacrylate
Thiolated CMC                       Thiolated polymer, etc.
Sodium CMC
HEC
HPC
HPMC
Methylhydroxyethylcellulose, etc.
According to water solubility
Water soluble                       Water insoluble

CMC, Thiolated CMC, Sodium Carbopol,Polycarbophil,
CMC, HEC, HPC,HPMC, MC, Polyacrylic acid, Polyacrylates
HPMC,PVA,PVP, etc.         Methacrylic acid, PEG, etc.




     According to charge
Cationic and Anionic                 Uncharged

Aminodextran, Chitosan,              Hydroxyethylated starch,
Chitosan-EDTA, Carbopol              HPC, PEG
Polycarbophil, Sodium alginate,      PVA, PVP, etc.
Pectin, Sodium CMC, CMC, etc.
Route/site          Bioadhesive formulation
Oral cavity (Buccal Tablet, Patch, Gel, Ointment,
and Sublingual)     Chewing gum, Hollow fibers
Nasal               Gel, Microspheres, Dry powders
Ocular              Insert, gel
Gastro intestinal   Gel, Tablet, Microspheres, Capsule,
                    Hollow fibers
Skin/Transdermal    Patch, Liposomes
Vaginal             Gel, Microspheres, Tablet
Rectal              Gel
 Bioadhesive tablets are immobilized drug delivery
  systems
 Formulated as monolithic, partially coated or
  multilayered matrices
 Formulation ingredients
1) API                         6) Sweetening agent
2) Mucoadhesive polymer        7) Flavoring agent
3) Permeation enhancer         8) Coloring agent
4) Diluent                     9) Buffering agent
5) Lubricant                  10) Backing layer
                                  polymers
Designs of bioadhesive tablets
   Small surface of contact with mucosa
   Lack of physical flexibility
   Difficult to obtain high release rate, which is
    required for some drugs
   The extent and frequency may cause irritation to
    mucosa
1)Weight variation
2) Thickness
3) Hardness
4) Friability
5) Drug content
6) Surface pH
7) In vitro drug release
8) In vitro drug permeation
9) Swelling study
10) Measurement of residence time / retention time
11) Adhesive strength determination
Measurement of residence time / retention time
 Provides quantitative information on mucoadhesive
  properties.
 The GI transit time of many mucoadhesives have been
  examined using radioisotopes .
  e.g. 51Cr and the time dependent distribution of the
  radioactivity in the GIT is measured.
 Esophageal bioadhesive property
  porcine oesophageal tissue is used.
 tissue is washed at a rate of 1ml/min


   with simulate saliva flow.
 1.5 mL of formulation was mixed with ~0.2 MBq Tc99m as a
   radioactive substance. Eluate is collected upto 30 min.
 fig : In-vitro apparatus used to measure the residence
       time to perticular tissue.
                                                  41
Measurement of mucoadhesive strength
Three different types of stress, tensile, shear and peel stress
 are measured
A) Tensile strength
B) Shear and Peel strength




C) Thumb test
 The adhesiveness is qualitatively measured by the
 difficulty of pulling the thumb from the adhesive as a
 function of the pressure and the contact time. It provides
 useful information on mucoadhesive potential
Bioadhesive drug delivery system
Dissolution of Buccal tablet:-




     fig : Mumtaz and Chang model for the dissolution of
     the buccal tablet.

    From the inlet dissolution medium is poured and from
     outlet it is collected and assayed.
 
                                                 45
   Gels includes bioadhesive gels and in situ forming gels
   Bioadhesive gels
 These   gels highly viscous semisolids prepared by using
  mucoadhesive polymers
 Formulated for various sites like buccal, nasal, vaginal,
  rectal,etc
 Formulation   ingredients of bioadhesive gel
1) Active pharmaceutical ingredient
2) Mucoadhesive polymer
3) Permeation enhancer
4) Preservative
5) Solvent
   In situ gels are in solution form and formed gels upon
    administration to particular site due to phase transition in
    environment of that site
   Gel formation is due to various mechanisms includes,
   Thermal change
   pH change
   change in electrolyte composition
   combination of any 2 mechanisms
Thermo    sensitive gel forming system
    Thermo sensitive polymer systems are formed from
aqueous polymer solutions with temperature changes
    Thermo sensitive polymers are copolymers of N-
isopropylacrylamide (PNiPAAM), polaxamer, etc.
    pH sensitive gel forming system
    pH sensitive gel forming systems, which swell or shrink
in response to changes in the pH
    Carbopol (polyacrylic acid) is mostly used as pH
sensitive polymer
 Ion  sensitive gel forming system
 Ion sensitive gel forming system is new type of gel, in
  which solution of polymer containing drug triggered to
  gel form when contact with specific ion at specific site
 Ion sensitive polymer includes sodium alginate, gellan
  gum, xyloglucan, carrageenan
 In situ gels formulate for various sites including nasal,
  ophthalmic, oral, vaginal, rectal
1) Drug content
2) Viscosity
3) pH
4) In vitro drug release
5)Adhesion properties: Adhesive strength is measured
  as described in tablets and the other methods are,
A)Membrane viscosity
 The     interaction between polymers and cell
  membranes was examined by labeling the cell
  membranes with fluorescent probes
 The   lipid bilayer and proteins of cell
  membranes were labeled with pyrene and
  fluorescein isothiocyanate
 The fluorescence spectrum of pyrene and the
  fluorescence depolarization of fluorescein
  isothiocyanate were used to examine the
  change in membrane viscosity after
  interaction with polymer
 It was assumed in this study that affinity of
  polymers to cell membranes is linearly
  related to the increase in membrane viscosity
B) Electrical conductance
 The adhesion of orabase, carbopol, guar gum, and
  methyl cellulose to artificial biomembrane in artificial
  saliva was studied by using a modified rotational
  viscometer capable of measuring electrical conductance
 In presence of adhesive material the conductance was
  comparatively low. As the adhesive was removed the
  value increased to final corresponding to conductance
  of saliva, which indicate the absence of adhesion
 Patches are designed for buccal delivery and transdermal
  delivery of drugs
 Buccal patches
 Designed either for unidirectional release or bidirectional
  release
 Use of impermeable backing layer will maximize the drug
  concentration gradient and prolong adhesion because the
  system is protected from saliva
 Typically size of such polymeric patches would be 1-3 cm 2 but
  may have dimensions as large as 10-15 cm2 depending on the
  site of administration
   Patch contains mucoadhesive polymer and supportive
    material




       Matrix system           Reservoir system
 Formulation ingredients of Buccal patch
1) API
2) Mucoadhesive polymer
3) Supporting material
4) Plasticizer
 Evaluation of Buccal patch

1) Thickness uniformity
2) Folding endurance
3) Uniformity of weight
4) Drug content uniformity
5) Swelling study
6) Surface pH
7) In vitro release study
8) Adhesive strength
 Transdermal patches
 Transdermal patch is a medicated adhesive placed on
  the skin to deliver a specific dose of medication
  through the skin and into bloodstream
 Formulation is same as buccal patches
 Evaluation of Transdermal patches

1) Thickness uniformity
2) Moisture content
3) Uniformity of weight
4) Drug content uniformity
5) Flatness study
6) Surface pH
7) In vitro release study
8) Adhesive strength
Mucoadhesion measurement by Modified balance method
   Chewing gums are mobile drug delivery systems
   The main target mucosa for drug absorption is sublingual
    mucosa
   Drug release is generally rapid but not as immediate as in case
    of fast dissolving tablets
   Commercially available medicated chewing gums are
    currently available for pain relief, smoking cessation, travel
    illness, and freshening of breath
   Medicated chewing gum offers advantages in comparison to
    conventional oral mucosal and oral dosage forms both for (a)
    local treatment of mouth diseases and (b) systemic effect after
    absorption through the buccal and sublingual mucosa or from
    the gastrointestinal tract
   Components of chewing gum

    Component              Concentration (%)


    Drug                   Max. approximately 50
    Gum base               20–40
    Bulk sweeteners        30-75
    Softeners              0-10
    Flavoring agents       1-5
    Coloring agents        ˂1
   Manufacturing process of chewing gum
 The  most common method comprises mixing the
  gum base with the other ingredients in a mixer with
  Z formed blades. The gum base can either be added
  in a solid form and softened through heating from
  the jacket of the mixer or from the frictional heat
  generated during the mixing process, or it can be
  added in a melted form.
 Chewing gum can also be manufactured by
  compression of powders or granulates on a
  conventional     tablet   machine     (compression
  technique).
   The release into saliva and disappears rapidly from the
    oral cavity because of involuntary swallowing
   The concentration drug in the oral cavity always tends to
    decrease as a result of salivary dilution
   The drug is not protected from the environment found in
    oral cavity
   Administration of such dosage form is restricted to short
    time periods because the delivery system in the oral
    cavity causes disturbance in drinking, eating and speaking
 Films are used for buccal bioadhesive drug delivery
 Both degradable and non-degradable forms of films have
  been developed
 The major method of polymeric film manufacture is the
  solvent evaporation process
 Formulation ingredients
1) API
2) Mucoadhesive polymer
3) Plasticizer
 Evaluation of film
1) Weight uniformity
2) Thickness
3) Swelling study
4) folding endurance
5) Drug content uniformity
6) Surface pH
7) In vitro drug release
8) Mucoadhesion study
   Solid ophthalmic delivery devices (inserts) are thin disks or
    small cylinders made with appropriate polymeric materials
    and fitting into the lower or upper conjuctival sac
   Their long persistence in the perocular area can result in a
    greater drug bioavailability with respect to liquid and
    semisolid formulations
   Mucoadhesive polymers can be profitably used as constituents
    of inserts to achieve prolonged contact with the conjuctival
    tissue
   Alternative approach for chewing gum formulations
   The design of micro porous hollow fiber of polysulphone
    intended for the delivery of histerelin, a LHRH agonist was
    reported (Burnside et al.)
   This fiber is intended to be placed in the buccal cavity for oral
    mucosal drug delivery
   The fiber may also prepare for periodontal application
   Multiparticulate system includes microspheres, liposomes and
    nanoparticles
Microspheres
 Bioadhesive microspheres include micro particles and
  microcapsules(size 1–1000µm in diameter)
 They have the potential to be used for targeted and controlled
  release drug delivery; but coupling of bioadhesive properties to
  microspheres has additional advantages,
 Efficient absorption and enhanced bioavailability of the drugs
  due to a high surface to volume ratio
 A much more intimate contact with the mucus layer
 Specific targeting of drugs to the absorption site
 Bioadhesive microspheres can be tailored to adhere to any
  mucosal tissue including those found in eye, nasal cavity,
  urinary and gastrointestinal tract, thus offering the possibilities
  of localized as well as systemic controlled release of drugs
 Their formulation contains API and mucoadhesive polymer
   Liposomes
 Liposomes are coated with mucoadhesive polymers and
  remain for longer period of time and improved the drug
  therapy
 Ocular route is widely used for mucoadhesive liposomal
  preparation
 Nanoparticles
 Nanoparticles prepared for mucoadhesive drug delivery by
  either consisting entirely of a bioadhesive polymer or having
  an outer coating of it
 Evaluation of multiparticulate system
1) Drug entrapment efficiency
2) Particle size analysis
3) In vitro release study
4) Mucoadhesion study

 Mucoadhesion study
In microspheres adhesion number is determined
 The adhesion number (Na) is,
                      Na = (N/No)*100
Where, No = total no. of applied particles
  N = no. of particles attached to the substrate
 Two methods for measurement
A)Falling liquid film method
B) Mucin gold staining
A)Falling liquid film method




The adhesion of particles to this surface is measured by
 passing the particle suspension over the surface and
 by comparing the fraction of particles adhered to the
 tissue
B) Mucin gold staining
 In this technique, colloid gold particles, which are red
  in solution, are stabilized by mucin molecules
 The interaction between mucin and adhesive particles is
  monitored by appearance of red color on surface.
EVALUATION OF BDDS
 IN VITRO / EX VIVO METHODS
a. Methods based on measurement of tensile strength.
b. Methods based on measurement of shear strength.
   OTHER IN VITRO METHODS
c. Adhesion weight method
d. Fluorescent probe method
e. Flow channel method
f. Falling liquid film method
g. Colloidal gold staining method
h. Mechanical spectroscopic method
I. Thumb test
j. Viscometric method
k. Adhesion number
   IN VIVO METHODS
 a. Use of radio isotopes
 b. Use of gamma scintigraphy
 In vivo evaluation methods
 In vivo methods used for evaluation are based on
   administration of polymers to a laboratory animal and
   tracking their transit through the GI system.
    Administration methods include forced oral gavage,
   surgical stomach implantation and infusion through a
   loop placed in situ in the small intestine. Tracking
   generally followed with the help of X-ray studies, radio
   opaque markers and radioactive elements etc.
 For e.g. X- ray studies for monitoring GI transit time for
   bioadhesive tablet made of BaSO4 and radiolabelled
   microspheres and nanoparticles.

                                                 73
   Ocular (Eye)
   Nasal cavity
   Oral (Buccal and Sublingual)
   Skin/Transdermal
   Gastro-intestinal and Colorectal
    (Colon+ Rectum)
   Vaginal
   The eye is one of the most important and complex
    organs of the body, because of its complicated anatomy
    many things can go wrong with the eye.
   Topical drug delivery systems to the eye can be very
    difficult to achieve because the eye has several
    protective mechanisms in place to get rid of foreign
    substances.
   An effective ocular drug delivery system must be easy
    to use, comfortable to the patient and maintain
    substantial concentrations of the drug in the eye to
    produce therapeutic effects.
   Problems associated with eye include conjunctivitis,
    Glaucoma and dry eye.
Ocular Bioadhesive Formulations
   GelTears® and Viscotears® Liquid gel eye drops
    are used for dry eye conditions and contain
    carbomer 980 (polyacrylic acid). Carbomers
    lubricate the eye by clinging to the surface of the
    eye. This can help reduce the frequency of their
    application into the eye.
   Pilogel® is an eye gel used in the treatment of
    glaucoma. It contains the high molecular weight
    polymer polyacrylic acid. The polymer increases
    the viscosity of the gel which provides a
    prolonged retention of the gel in the eye.
   Drugs such as antihistamines and steroids are
    administered as nasal drops or nasal sprays to treat
    conditions affecting the nose. However nasal
    mucociliary clearance affects the retention and
    therefore the effects of the drugs in the nose.
   The effects of bioadhesive polymers on mucociliary
    clearance was examined by Zhou and Donovan
    (1996).
   Methylcellulose exhibited the most reduction in
    mucociliary clearance whilst Carbopol 934P showed
    the least reduction in mucociliary clearance in the rats
    used.
Bioadhesive formulations for Nasal cavity
   Rhinocort® Nasal spray is a powdered mixture of the steroid
    Beclomethasone dipropionate(50μg) and 30mg of Hydroxypropyl
    cellulose(HPC).
   Used for patients suffering from nasal allergy.
   The powder sticks to and swells on the cells lining the nose and remains
    there for about 6 hrs.
   Beconase® Nasal spray is used to treat nasal inflammation and nasal
    allergies associated with hayfever.
   It contains the active ingredient Beclometasone dipropionate and the
    bioadhesive polymers carboxymethyl cellulose and microcrystalline
    cellulose.
   Nasacort® Nasal spray is used to treat allergies that result in
    inflammation of the nose. The active ingredient in this product is
    Triamcinolone acetonide as well as the bioadhesive polymer
    microcrystalline cellulose. The polymer swells in the presence of water
    and is able to spread across the nasal mucosa thus helping the
    distribution of the drug over the mucosal surface.
Bioadhesive drug delivery system
   The oral cavity or the mouth comprises of the cheeks, teeth
    and the tongue.
   It is an entrance of the digestive system and plays many
    important functions which include chewing, speaking and
    tasting.
   Some of these functions are impaired by diseases such as
    ulcers, microbial infections and inflammation.
Examples of products
   Corlan®: Corlan pellets are used in the
     treatment of mouth ulcers to reduce the pain, swelling and
    inflammation associated with mouth ulcers.
   The active ingredient of the pellet is Hydrocortisone
    succinate. It also contains the bioadhesive polymer Acacia
    which helps prolong the effect of the drug in the oral cavity.
The Buccal Mucosa
   Buccastem® is a drug used in the treatment of nausea,
    vomiting and vertigo. It contains the bioadhesive agents
    Polyvinylpyrrolidone and Xanthan gum.
   Suscard® is a buccal tablet used in the treatment of angina.
    It contains the bioadhesive agent Hydroxypropyl
    methylcellulose (HPMC).
The sublingual mucosa
   Drugs administered via the sublingual route are formulated
    as tablets, powders, solutions or aerosol sprays.
   Examples of sublingual products include Glyceryl
    Trinitrate (GTN) aerosol spray and tablet which is
    administered under the tongue for the prophylactic
    treatment of angina.
 The skin is the outer covering of the body and consists of
  different layers. It performs several functions which
  include:
   Protecting the body from injury and invasion by
    pathogens
   Preventing the body from becoming dehydrated
   Regulating body temperature
   Production of Vitamin D
 Topical Bioadhesive Formulations
 The drug delivery systems used in this case are required to
  adhere to the skin for the purpose of:
   Collecting body fluids
   Protecting the skin
   Providing local or systemic drug delivery
Transdermal Bioadhesive formulations
   Voltarol Emulgel: This is a gel which provides a local
    relief from pain and inflammation in the tendons,
    muscles and joints.
   It contains the bioadhesive polymer carbomer which
    aids the absorption of the active drug by spreading it
    into the affected area.
   Feldene: This gel is used in the treatment of
    conditions which are characterised by pain,
    inflammation and stiffness.
   The active ingredient in this formulation is piroxicam
    but the gel also contains two bioadhesive agents to
    increase its retention at the absorption site. These
    agents are Carbopol 980 and hydroxyethyl cellulose.
   The rectum is the terminal or end portion of the
    gastrointestinal tract. It is an important route of
    administration for drugs that have severe
    gastrointestinal side effects.
   This route is also suitable for patients who cannot take
    medicines via the oral route such as unconscious
    patients and infants.
   The drugs absorbed from the rectum can escape
    breakdown by hepatic enzymes. For this reason
    mucoadhesive suppositories have been developed for
    the local treatment of diseases such as haemorrhoids
    and rectal cancer.
Rectal Bioadhesive Formulations
   Anacal® is a rectal ointment used to relieve the
    symptoms associated with haemorrhoids. It
    contains the bioadhesive agent polyethylene high
    polymer 1500.
   Germoloids® is a rectal ointment used to relief the
    pain, swelling, itchiness and irritation associated
    with haemorrhoids. It contains the polymer
    propylene glycol.
 The vagina is the lower part of the female reproductive tract.
 It is a muscular tube lined with mucous membrane which is
  covered with a layer of stratified squamous epithelium with an
  underlying layer of connective tissue (lamina propria)
Common conditions affecting the vagina
 The epithelium of the vagina contains glycogen, which is
  broken down enzymes and bacteria into acids such as lactic
  acid. This maintains a low vaginal pH which is normally
  between 4 and 5.
 Such a pH is desirable because it makes the vagina
  inhospitable to pathogens.
 Decreased levels of glycogen in the vagina leads to an increase
  in vaginal pH and makes the vagina more susceptible to
  infection such as Vaginitis, Bacterial vaginosis, Candidiasis
  (Thrush), Trichomoniasis etc..
Vaginal bioadhesive formulations
   The intravaginal route has been used to deliver contraceptives as
    well as anti-infective agents such as antifungal drugs to exert a
    local effect.
   Agents targeted for the vaginal route have been formulated into
    various dosage forms including creams, gels and vaginal tablets.
   Bioadhesive polymers are incorporated into vaginal formulations
    to aid the adhering of the dosage form to its target site.
   Polymers also increase the retention of the active drug in the
    vagina and also optimise the spread of the formulation over the
    vaginal epithelium.
   S-DBMP-T(Slowly Disintegrating
    Buccal Mucoadhesive Plain-Tablet)
   BCTS (Buccal Covered-Tablet System)
   VagiSiteTM Bioadhesive Technology
   Iga et al. developed this system
   S-DBMP-T are prepared by incorporating a relatively
    large amount of hydroxypropylcellulose in a tablet
    formulation
   An example of a typical composition is a tablet
    composed of 20 mg of drug, 20 mg of
    hydroxypropylcellulose,          20     mg         of
    carboxymethylcellulose       (ECG-505, disintegrating
    agent), and 60 mg of lactose
   The S-DBMP-T technology was originally developed
    for increasing the bioavailability of oxendolone (a
    steroidal anti-androgen)
   To maintain the tablet shape for as long as possible, Iga
    et al. developed a method to restrict disintegration from
    the sides of the tablets
   The method involved sandwiching a S-DBMP-T tablet
    between two polyethylene sheets. The upper sheet
    contained a hole that allowed the tablet to absorb water
    and disintegrate only through the hole. The lower sheet
    contained adhesives to allow the delivery system to
    adhere to the gingiva for a long time.
   Developed by KV Pharmaceutical Company, St. Louis,
    Missouri, U.S.A.
   The VagiSiteTM technology comprises a high-internal-phase-
    ratio, water-in-oil emulsion
   The internal phase of the emulsion acts as the carrier of the
    active drug. The drug-laden internal-dispersed phase globules
    serve a dual purpose for both the sequestering and the
    controlled release of the active agent, butoconazole nitrate
   After introduction of the drug-containing emulsion to a
    mucosal surface, in this case the vaginal mucosa, a thin
    bioadhesive film of contiguous drug-laden internal-phase
    globules forms on the mucosal surface
   Rathbone MJ et al., Modified Release Drug Delivery
    Technology, Marcel Dekker, Inc., 2002, 349-81, 801-6
   Vyas SP, Khar RK., Controlled Drug Delivery: Concepts and
    Advances, Vallabh Prakashan, First Edition: 2002, 257-314
   Methiowitz E et al., Bioadhesive Drug Delivery System,
    Marcel Dekker, Inc., 1999, 551-3, 621-31
   Andrews GP et al., Mucoadhesive polymeric platforms for
    controlled drug delivery, European Journal of Pharmaceutics
    and Biopharmaceutics 71 (2009) 505–18
   Salamat-Miller N et al., The use of mucoadhesive polymers in
    buccal drug delivery, Advanced Drug Delivery Reviews 57
    (2005) 1666– 91

More Related Content

What's hot

Buccal drug delivery system
Buccal drug delivery systemBuccal drug delivery system
Buccal drug delivery systemshivamthakore
 
Controlled drug delivery systems
Controlled drug delivery systemsControlled drug delivery systems
Controlled drug delivery systemsTheabhi.in
 
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)Factors affecting design of Controlled Release Drug Delivery Systems (write-up)
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)Suraj Choudhary
 
Controlled Release Drug Delivery Systems - Types, Methods and Applications
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsControlled Release Drug Delivery Systems - Types, Methods and Applications
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsSuraj Choudhary
 
Gastro Retentive Drug Delivery System
Gastro Retentive Drug Delivery SystemGastro Retentive Drug Delivery System
Gastro Retentive Drug Delivery SystemDr Gajanan Sanap
 
Transdermal Drug Delivery System (TDDS)
Transdermal Drug Delivery System (TDDS)Transdermal Drug Delivery System (TDDS)
Transdermal Drug Delivery System (TDDS)PRABU12345678
 
microspheres types , preparation and evaluation
microspheres types , preparation and evaluationmicrospheres types , preparation and evaluation
microspheres types , preparation and evaluationSowjanya
 
Controlled release drug delivery system
Controlled release drug delivery system Controlled release drug delivery system
Controlled release drug delivery system MOHAMMEDABDULSALAM32
 
Approaches to Targeted Delivery of Drugs
Approaches to Targeted Delivery of DrugsApproaches to Targeted Delivery of Drugs
Approaches to Targeted Delivery of Drugswonderingsoul114
 
Occular drug delivery system ppt
Occular drug delivery system pptOccular drug delivery system ppt
Occular drug delivery system pptPankaj Verma
 
Implantable Drug Delivery System
Implantable Drug Delivery SystemImplantable Drug Delivery System
Implantable Drug Delivery Systemparesh bharodiya
 
MUCOADHESIIVE DRUG DELIVERY SYSTEM
MUCOADHESIIVE DRUG DELIVERY SYSTEMMUCOADHESIIVE DRUG DELIVERY SYSTEM
MUCOADHESIIVE DRUG DELIVERY SYSTEMDr Gajanan Sanap
 
Transdermal drug delivery system ppt
Transdermal drug delivery system pptTransdermal drug delivery system ppt
Transdermal drug delivery system pptDeepak Sarangi
 
Approaches Of Gastro-Retentive Drug Delivery System or GRDDS
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSApproaches Of Gastro-Retentive Drug Delivery System or GRDDS
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
 
Mucoadhesive drug delivery system Mali vv ppt
Mucoadhesive drug delivery system Mali vv pptMucoadhesive drug delivery system Mali vv ppt
Mucoadhesive drug delivery system Mali vv pptVidhyaMali1
 
Formulation and evaluation of tdds
Formulation and evaluation of tddsFormulation and evaluation of tdds
Formulation and evaluation of tddsPankaj Verma
 
buccal drug delivery system
buccal drug delivery systembuccal drug delivery system
buccal drug delivery systemrasikawalunj
 
Transdermal drug delivery system
Transdermal drug delivery systemTransdermal drug delivery system
Transdermal drug delivery systemArshad Khan
 

What's hot (20)

Buccal drug delivery system
Buccal drug delivery systemBuccal drug delivery system
Buccal drug delivery system
 
Controlled drug delivery systems
Controlled drug delivery systemsControlled drug delivery systems
Controlled drug delivery systems
 
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)Factors affecting design of Controlled Release Drug Delivery Systems (write-up)
Factors affecting design of Controlled Release Drug Delivery Systems (write-up)
 
Gastroretentive Drug Delivery System
Gastroretentive Drug Delivery SystemGastroretentive Drug Delivery System
Gastroretentive Drug Delivery System
 
Controlled Release Drug Delivery Systems - Types, Methods and Applications
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsControlled Release Drug Delivery Systems - Types, Methods and Applications
Controlled Release Drug Delivery Systems - Types, Methods and Applications
 
Gastro Retentive Drug Delivery System
Gastro Retentive Drug Delivery SystemGastro Retentive Drug Delivery System
Gastro Retentive Drug Delivery System
 
Transdermal Drug Delivery System (TDDS)
Transdermal Drug Delivery System (TDDS)Transdermal Drug Delivery System (TDDS)
Transdermal Drug Delivery System (TDDS)
 
microspheres types , preparation and evaluation
microspheres types , preparation and evaluationmicrospheres types , preparation and evaluation
microspheres types , preparation and evaluation
 
Nasal and pulmonary dds
Nasal and pulmonary ddsNasal and pulmonary dds
Nasal and pulmonary dds
 
Controlled release drug delivery system
Controlled release drug delivery system Controlled release drug delivery system
Controlled release drug delivery system
 
Approaches to Targeted Delivery of Drugs
Approaches to Targeted Delivery of DrugsApproaches to Targeted Delivery of Drugs
Approaches to Targeted Delivery of Drugs
 
Occular drug delivery system ppt
Occular drug delivery system pptOccular drug delivery system ppt
Occular drug delivery system ppt
 
Implantable Drug Delivery System
Implantable Drug Delivery SystemImplantable Drug Delivery System
Implantable Drug Delivery System
 
MUCOADHESIIVE DRUG DELIVERY SYSTEM
MUCOADHESIIVE DRUG DELIVERY SYSTEMMUCOADHESIIVE DRUG DELIVERY SYSTEM
MUCOADHESIIVE DRUG DELIVERY SYSTEM
 
Transdermal drug delivery system ppt
Transdermal drug delivery system pptTransdermal drug delivery system ppt
Transdermal drug delivery system ppt
 
Approaches Of Gastro-Retentive Drug Delivery System or GRDDS
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSApproaches Of Gastro-Retentive Drug Delivery System or GRDDS
Approaches Of Gastro-Retentive Drug Delivery System or GRDDS
 
Mucoadhesive drug delivery system Mali vv ppt
Mucoadhesive drug delivery system Mali vv pptMucoadhesive drug delivery system Mali vv ppt
Mucoadhesive drug delivery system Mali vv ppt
 
Formulation and evaluation of tdds
Formulation and evaluation of tddsFormulation and evaluation of tdds
Formulation and evaluation of tdds
 
buccal drug delivery system
buccal drug delivery systembuccal drug delivery system
buccal drug delivery system
 
Transdermal drug delivery system
Transdermal drug delivery systemTransdermal drug delivery system
Transdermal drug delivery system
 

Viewers also liked

Bio Adhesive Drug Delivery System
Bio Adhesive Drug Delivery SystemBio Adhesive Drug Delivery System
Bio Adhesive Drug Delivery Systemoptimpharma
 
Mucoadhesive drug delivery system
Mucoadhesive drug delivery system Mucoadhesive drug delivery system
Mucoadhesive drug delivery system Sonam Gandhi
 
Bioadhesive drug delivery system
Bioadhesive drug delivery systemBioadhesive drug delivery system
Bioadhesive drug delivery systemSunil Boreddy Rx
 
Mucoadhesive drug delivery system
Mucoadhesive drug delivery system   Mucoadhesive drug delivery system
Mucoadhesive drug delivery system Sonam Gandhi
 
Muccoadhesive drug delivery system
Muccoadhesive drug delivery systemMuccoadhesive drug delivery system
Muccoadhesive drug delivery systemGaurav Kr
 
Buccal drug delivery system
Buccal drug delivery systemBuccal drug delivery system
Buccal drug delivery systemShivaram
 
Buccal &Sublingual Drug Delivery System
Buccal &Sublingual Drug Delivery SystemBuccal &Sublingual Drug Delivery System
Buccal &Sublingual Drug Delivery SystemAshish Motivaras
 
Buccal and sublingual drug delivery system
Buccal and sublingual drug delivery systemBuccal and sublingual drug delivery system
Buccal and sublingual drug delivery systemSagar Savale
 
Nasal Drug Delivery System
Nasal Drug Delivery SystemNasal Drug Delivery System
Nasal Drug Delivery SystemKawitha
 
buccal drug delivery system
buccal drug delivery systembuccal drug delivery system
buccal drug delivery systemDanish Kurien
 
Buccal bioadhesive drug delivery system G1ppt
Buccal bioadhesive drug delivery system G1pptBuccal bioadhesive drug delivery system G1ppt
Buccal bioadhesive drug delivery system G1pptPadi Jeevanreddy
 
NASAL DRUG DELIVERY SYSTEM
NASAL DRUG DELIVERY SYSTEMNASAL DRUG DELIVERY SYSTEM
NASAL DRUG DELIVERY SYSTEMPrajakta Chavan
 
oral controlled drug delivery system
oral controlled drug delivery systemoral controlled drug delivery system
oral controlled drug delivery systemBaliram Musale
 
Controlled release mucoadhesive microcapsules using various polymers and tech...
Controlled release mucoadhesive microcapsules using various polymers and tech...Controlled release mucoadhesive microcapsules using various polymers and tech...
Controlled release mucoadhesive microcapsules using various polymers and tech...srirampharma
 
Polymer microspheres for controlled drug release
Polymer microspheres for controlled drug releasePolymer microspheres for controlled drug release
Polymer microspheres for controlled drug releaseDuwan Arismendy
 
Activation Controlled drug Delivery System
Activation Controlled drug Delivery SystemActivation Controlled drug Delivery System
Activation Controlled drug Delivery SystemSuraj Choudhary
 

Viewers also liked (20)

Bio Adhesive Drug Delivery System
Bio Adhesive Drug Delivery SystemBio Adhesive Drug Delivery System
Bio Adhesive Drug Delivery System
 
Mucoadhesive drug delivery system
Mucoadhesive drug delivery system Mucoadhesive drug delivery system
Mucoadhesive drug delivery system
 
MUCOADHESIVE DRUD DELIVERY SYSTEM
MUCOADHESIVE DRUD DELIVERY SYSTEM MUCOADHESIVE DRUD DELIVERY SYSTEM
MUCOADHESIVE DRUD DELIVERY SYSTEM
 
Bioadhesive drug delivery system
Bioadhesive drug delivery systemBioadhesive drug delivery system
Bioadhesive drug delivery system
 
Mucoadhesive drug delivery system
Mucoadhesive drug delivery system   Mucoadhesive drug delivery system
Mucoadhesive drug delivery system
 
Muccoadhesive drug delivery system
Muccoadhesive drug delivery systemMuccoadhesive drug delivery system
Muccoadhesive drug delivery system
 
Buccal drug delivery system
Buccal drug delivery systemBuccal drug delivery system
Buccal drug delivery system
 
Buccal &Sublingual Drug Delivery System
Buccal &Sublingual Drug Delivery SystemBuccal &Sublingual Drug Delivery System
Buccal &Sublingual Drug Delivery System
 
Nasal drug delivery
Nasal drug deliveryNasal drug delivery
Nasal drug delivery
 
Buccal and sublingual drug delivery system
Buccal and sublingual drug delivery systemBuccal and sublingual drug delivery system
Buccal and sublingual drug delivery system
 
Nasal Drug Delivery System
Nasal Drug Delivery SystemNasal Drug Delivery System
Nasal Drug Delivery System
 
buccal drug delivery system
buccal drug delivery systembuccal drug delivery system
buccal drug delivery system
 
Buccal bioadhesive drug delivery system G1ppt
Buccal bioadhesive drug delivery system G1pptBuccal bioadhesive drug delivery system G1ppt
Buccal bioadhesive drug delivery system G1ppt
 
NASAL DRUG DELIVERY SYSTEM
NASAL DRUG DELIVERY SYSTEMNASAL DRUG DELIVERY SYSTEM
NASAL DRUG DELIVERY SYSTEM
 
oral controlled drug delivery system
oral controlled drug delivery systemoral controlled drug delivery system
oral controlled drug delivery system
 
Controlled Release Oral Drug Delivery System
Controlled Release Oral Drug Delivery SystemControlled Release Oral Drug Delivery System
Controlled Release Oral Drug Delivery System
 
Controlled release mucoadhesive microcapsules using various polymers and tech...
Controlled release mucoadhesive microcapsules using various polymers and tech...Controlled release mucoadhesive microcapsules using various polymers and tech...
Controlled release mucoadhesive microcapsules using various polymers and tech...
 
Bio adhesive dds
Bio adhesive ddsBio adhesive dds
Bio adhesive dds
 
Polymer microspheres for controlled drug release
Polymer microspheres for controlled drug releasePolymer microspheres for controlled drug release
Polymer microspheres for controlled drug release
 
Activation Controlled drug Delivery System
Activation Controlled drug Delivery SystemActivation Controlled drug Delivery System
Activation Controlled drug Delivery System
 

Similar to Bioadhesive drug delivery system

Buccal drug delivery system 1 new
Buccal drug delivery system 1 newBuccal drug delivery system 1 new
Buccal drug delivery system 1 newSNEHADAS123
 
Mucosal Drug Delivery System
Mucosal Drug Delivery SystemMucosal Drug Delivery System
Mucosal Drug Delivery SystemSwatiSen3
 
Mucoadhesive drug delivery system
Mucoadhesive drug delivery systemMucoadhesive drug delivery system
Mucoadhesive drug delivery systemRavish Yadav
 
Mucosal Drug Delivery System.pptx
Mucosal Drug Delivery System.pptxMucosal Drug Delivery System.pptx
Mucosal Drug Delivery System.pptxAkshataJain17
 
Oral mucosal drug delivery systems
Oral mucosal drug delivery systemsOral mucosal drug delivery systems
Oral mucosal drug delivery systemsMEENAL VERMA
 
Buccal drug delivery pptx
Buccal drug delivery pptxBuccal drug delivery pptx
Buccal drug delivery pptxSreedhar Reddy
 
Mucosal drug delivery system.pdf
Mucosal drug delivery system.pdfMucosal drug delivery system.pdf
Mucosal drug delivery system.pdfAkankshaPatel55
 
Mucosal drug delivery system novel drug delivery system
Mucosal drug delivery system novel drug delivery systemMucosal drug delivery system novel drug delivery system
Mucosal drug delivery system novel drug delivery systemShubhangiKhade7
 
TOPIC- MUCOADHESIVE DRUG DELIVERY SYSYTEM.pptx
TOPIC- MUCOADHESIVE DRUG  DELIVERY SYSYTEM.pptxTOPIC- MUCOADHESIVE DRUG  DELIVERY SYSYTEM.pptx
TOPIC- MUCOADHESIVE DRUG DELIVERY SYSYTEM.pptxSAURABH PUNIA
 
Bio/Mucoadhesive drug deivery system
Bio/Mucoadhesive drug deivery systemBio/Mucoadhesive drug deivery system
Bio/Mucoadhesive drug deivery systemSwapnil Singh
 
Buccal drug delivery system
Buccal drug delivery systemBuccal drug delivery system
Buccal drug delivery systemSiddu K M
 
Buccal drug delivery systems
Buccal drug delivery systemsBuccal drug delivery systems
Buccal drug delivery systemshardik dhiman
 
Buccal drug delivery systems
Buccal drug delivery systemsBuccal drug delivery systems
Buccal drug delivery systemshardik dhiman
 
Formulation and invitro evaluation of microspheres
Formulation and invitro evaluation of  microspheresFormulation and invitro evaluation of  microspheres
Formulation and invitro evaluation of microspheresTejaswi Kurma
 
Formulation and invitro evaluation of microspheres
Formulation and invitro evaluation of  microspheresFormulation and invitro evaluation of  microspheres
Formulation and invitro evaluation of microspheresTejaswi Kurma
 
buccal drug delivery how to deliver drug
buccal drug delivery how to deliver drugbuccal drug delivery how to deliver drug
buccal drug delivery how to deliver drugamartya2087
 
2103313001_dhavalkumar H rathod_MPH102T.pptx
2103313001_dhavalkumar H rathod_MPH102T.pptx2103313001_dhavalkumar H rathod_MPH102T.pptx
2103313001_dhavalkumar H rathod_MPH102T.pptxMariyambibiMandarawa1
 
Novel drug delivery system.various factor affecting the design of mucoadhesive
Novel drug delivery system.various factor affecting the design of mucoadhesiveNovel drug delivery system.various factor affecting the design of mucoadhesive
Novel drug delivery system.various factor affecting the design of mucoadhesiveSusmitaGhosh94
 

Similar to Bioadhesive drug delivery system (20)

Buccal drug delivery system 1 new
Buccal drug delivery system 1 newBuccal drug delivery system 1 new
Buccal drug delivery system 1 new
 
Mucosal Drug Delivery System
Mucosal Drug Delivery SystemMucosal Drug Delivery System
Mucosal Drug Delivery System
 
Mucoadhesive drug delivery system
Mucoadhesive drug delivery systemMucoadhesive drug delivery system
Mucoadhesive drug delivery system
 
Mucosal Drug Delivery System.pptx
Mucosal Drug Delivery System.pptxMucosal Drug Delivery System.pptx
Mucosal Drug Delivery System.pptx
 
Oral mucosal drug delivery systems
Oral mucosal drug delivery systemsOral mucosal drug delivery systems
Oral mucosal drug delivery systems
 
Buccal drug delivery pptx
Buccal drug delivery pptxBuccal drug delivery pptx
Buccal drug delivery pptx
 
Mucosal drug delivery system.pdf
Mucosal drug delivery system.pdfMucosal drug delivery system.pdf
Mucosal drug delivery system.pdf
 
Mucosal drug delivery system novel drug delivery system
Mucosal drug delivery system novel drug delivery systemMucosal drug delivery system novel drug delivery system
Mucosal drug delivery system novel drug delivery system
 
TOPIC- MUCOADHESIVE DRUG DELIVERY SYSYTEM.pptx
TOPIC- MUCOADHESIVE DRUG  DELIVERY SYSYTEM.pptxTOPIC- MUCOADHESIVE DRUG  DELIVERY SYSYTEM.pptx
TOPIC- MUCOADHESIVE DRUG DELIVERY SYSYTEM.pptx
 
Bio/Mucoadhesive drug deivery system
Bio/Mucoadhesive drug deivery systemBio/Mucoadhesive drug deivery system
Bio/Mucoadhesive drug deivery system
 
Bioadhesion Drug Delivery system
Bioadhesion Drug Delivery systemBioadhesion Drug Delivery system
Bioadhesion Drug Delivery system
 
Buccal drug delivery system
Buccal drug delivery systemBuccal drug delivery system
Buccal drug delivery system
 
Bioadhesives in drug delivery
Bioadhesives in drug deliveryBioadhesives in drug delivery
Bioadhesives in drug delivery
 
Buccal drug delivery systems
Buccal drug delivery systemsBuccal drug delivery systems
Buccal drug delivery systems
 
Buccal drug delivery systems
Buccal drug delivery systemsBuccal drug delivery systems
Buccal drug delivery systems
 
Formulation and invitro evaluation of microspheres
Formulation and invitro evaluation of  microspheresFormulation and invitro evaluation of  microspheres
Formulation and invitro evaluation of microspheres
 
Formulation and invitro evaluation of microspheres
Formulation and invitro evaluation of  microspheresFormulation and invitro evaluation of  microspheres
Formulation and invitro evaluation of microspheres
 
buccal drug delivery how to deliver drug
buccal drug delivery how to deliver drugbuccal drug delivery how to deliver drug
buccal drug delivery how to deliver drug
 
2103313001_dhavalkumar H rathod_MPH102T.pptx
2103313001_dhavalkumar H rathod_MPH102T.pptx2103313001_dhavalkumar H rathod_MPH102T.pptx
2103313001_dhavalkumar H rathod_MPH102T.pptx
 
Novel drug delivery system.various factor affecting the design of mucoadhesive
Novel drug delivery system.various factor affecting the design of mucoadhesiveNovel drug delivery system.various factor affecting the design of mucoadhesive
Novel drug delivery system.various factor affecting the design of mucoadhesive
 

More from Dr. Shreeraj Shah

More from Dr. Shreeraj Shah (8)

Recent advances in GRDDS
Recent advances in GRDDSRecent advances in GRDDS
Recent advances in GRDDS
 
Niosome
Niosome Niosome
Niosome
 
Detailed study of the equipments as per sch m
Detailed study of the equipments as per sch mDetailed study of the equipments as per sch m
Detailed study of the equipments as per sch m
 
Intelligent drug delivery system
Intelligent drug delivery systemIntelligent drug delivery system
Intelligent drug delivery system
 
Tailor made medicine
Tailor made medicineTailor made medicine
Tailor made medicine
 
Sonophoresis
Sonophoresis Sonophoresis
Sonophoresis
 
Iontophoresis
Iontophoresis Iontophoresis
Iontophoresis
 
Insitu gel drug delivery system
Insitu gel drug delivery systemInsitu gel drug delivery system
Insitu gel drug delivery system
 

Recently uploaded

Optical Fibre and It's Applications.pptx
Optical Fibre and It's Applications.pptxOptical Fibre and It's Applications.pptx
Optical Fibre and It's Applications.pptxPurva Nikam
 
Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...
Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...
Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...Dr. Asif Anas
 
How to Show Error_Warning Messages in Odoo 17
How to Show Error_Warning Messages in Odoo 17How to Show Error_Warning Messages in Odoo 17
How to Show Error_Warning Messages in Odoo 17Celine George
 
Easter in the USA presentation by Chloe.
Easter in the USA presentation by Chloe.Easter in the USA presentation by Chloe.
Easter in the USA presentation by Chloe.EnglishCEIPdeSigeiro
 
How to Send Emails From Odoo 17 Using Code
How to Send Emails From Odoo 17 Using CodeHow to Send Emails From Odoo 17 Using Code
How to Send Emails From Odoo 17 Using CodeCeline George
 
Slides CapTechTalks Webinar March 2024 Joshua Sinai.pptx
Slides CapTechTalks Webinar March 2024 Joshua Sinai.pptxSlides CapTechTalks Webinar March 2024 Joshua Sinai.pptx
Slides CapTechTalks Webinar March 2024 Joshua Sinai.pptxCapitolTechU
 
Vani Magazine - Quarterly Magazine of Seshadripuram Educational Trust
Vani Magazine - Quarterly Magazine of Seshadripuram Educational TrustVani Magazine - Quarterly Magazine of Seshadripuram Educational Trust
Vani Magazine - Quarterly Magazine of Seshadripuram Educational TrustSavipriya Raghavendra
 
Clinical Pharmacy Introduction to Clinical Pharmacy, Concept of clinical pptx
Clinical Pharmacy  Introduction to Clinical Pharmacy, Concept of clinical pptxClinical Pharmacy  Introduction to Clinical Pharmacy, Concept of clinical pptx
Clinical Pharmacy Introduction to Clinical Pharmacy, Concept of clinical pptxraviapr7
 
5 charts on South Africa as a source country for international student recrui...
5 charts on South Africa as a source country for international student recrui...5 charts on South Africa as a source country for international student recrui...
5 charts on South Africa as a source country for international student recrui...CaraSkikne1
 
Quality Assurance_GOOD LABORATORY PRACTICE
Quality Assurance_GOOD LABORATORY PRACTICEQuality Assurance_GOOD LABORATORY PRACTICE
Quality Assurance_GOOD LABORATORY PRACTICESayali Powar
 
Patient Counselling. Definition of patient counseling; steps involved in pati...
Patient Counselling. Definition of patient counseling; steps involved in pati...Patient Counselling. Definition of patient counseling; steps involved in pati...
Patient Counselling. Definition of patient counseling; steps involved in pati...raviapr7
 
KARNAADA.pptx made by - saransh dwivedi ( SD ) - SHALAKYA TANTRA - ENT - 4...
KARNAADA.pptx  made by -  saransh dwivedi ( SD ) -  SHALAKYA TANTRA - ENT - 4...KARNAADA.pptx  made by -  saransh dwivedi ( SD ) -  SHALAKYA TANTRA - ENT - 4...
KARNAADA.pptx made by - saransh dwivedi ( SD ) - SHALAKYA TANTRA - ENT - 4...M56BOOKSTORE PRODUCT/SERVICE
 
Over the counter (OTC)- Sale, rational use.pptx
Over the counter (OTC)- Sale, rational use.pptxOver the counter (OTC)- Sale, rational use.pptx
Over the counter (OTC)- Sale, rational use.pptxraviapr7
 
How to Manage Cross-Selling in Odoo 17 Sales
How to Manage Cross-Selling in Odoo 17 SalesHow to Manage Cross-Selling in Odoo 17 Sales
How to Manage Cross-Selling in Odoo 17 SalesCeline George
 
In - Vivo and In - Vitro Correlation.pptx
In - Vivo and In - Vitro Correlation.pptxIn - Vivo and In - Vitro Correlation.pptx
In - Vivo and In - Vitro Correlation.pptxAditiChauhan701637
 
Drug Information Services- DIC and Sources.
Drug Information Services- DIC and Sources.Drug Information Services- DIC and Sources.
Drug Information Services- DIC and Sources.raviapr7
 
HED Office Sohayok Exam Question Solution 2023.pdf
HED Office Sohayok Exam Question Solution 2023.pdfHED Office Sohayok Exam Question Solution 2023.pdf
HED Office Sohayok Exam Question Solution 2023.pdfMohonDas
 
DUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRA
DUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRADUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRA
DUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRATanmoy Mishra
 
How to Create a Toggle Button in Odoo 17
How to Create a Toggle Button in Odoo 17How to Create a Toggle Button in Odoo 17
How to Create a Toggle Button in Odoo 17Celine George
 
Protein Structure - threading Protein modelling pptx
Protein Structure - threading Protein modelling pptxProtein Structure - threading Protein modelling pptx
Protein Structure - threading Protein modelling pptxvidhisharma994099
 

Recently uploaded (20)

Optical Fibre and It's Applications.pptx
Optical Fibre and It's Applications.pptxOptical Fibre and It's Applications.pptx
Optical Fibre and It's Applications.pptx
 
Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...
Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...
Unveiling the Intricacies of Leishmania donovani: Structure, Life Cycle, Path...
 
How to Show Error_Warning Messages in Odoo 17
How to Show Error_Warning Messages in Odoo 17How to Show Error_Warning Messages in Odoo 17
How to Show Error_Warning Messages in Odoo 17
 
Easter in the USA presentation by Chloe.
Easter in the USA presentation by Chloe.Easter in the USA presentation by Chloe.
Easter in the USA presentation by Chloe.
 
How to Send Emails From Odoo 17 Using Code
How to Send Emails From Odoo 17 Using CodeHow to Send Emails From Odoo 17 Using Code
How to Send Emails From Odoo 17 Using Code
 
Slides CapTechTalks Webinar March 2024 Joshua Sinai.pptx
Slides CapTechTalks Webinar March 2024 Joshua Sinai.pptxSlides CapTechTalks Webinar March 2024 Joshua Sinai.pptx
Slides CapTechTalks Webinar March 2024 Joshua Sinai.pptx
 
Vani Magazine - Quarterly Magazine of Seshadripuram Educational Trust
Vani Magazine - Quarterly Magazine of Seshadripuram Educational TrustVani Magazine - Quarterly Magazine of Seshadripuram Educational Trust
Vani Magazine - Quarterly Magazine of Seshadripuram Educational Trust
 
Clinical Pharmacy Introduction to Clinical Pharmacy, Concept of clinical pptx
Clinical Pharmacy  Introduction to Clinical Pharmacy, Concept of clinical pptxClinical Pharmacy  Introduction to Clinical Pharmacy, Concept of clinical pptx
Clinical Pharmacy Introduction to Clinical Pharmacy, Concept of clinical pptx
 
5 charts on South Africa as a source country for international student recrui...
5 charts on South Africa as a source country for international student recrui...5 charts on South Africa as a source country for international student recrui...
5 charts on South Africa as a source country for international student recrui...
 
Quality Assurance_GOOD LABORATORY PRACTICE
Quality Assurance_GOOD LABORATORY PRACTICEQuality Assurance_GOOD LABORATORY PRACTICE
Quality Assurance_GOOD LABORATORY PRACTICE
 
Patient Counselling. Definition of patient counseling; steps involved in pati...
Patient Counselling. Definition of patient counseling; steps involved in pati...Patient Counselling. Definition of patient counseling; steps involved in pati...
Patient Counselling. Definition of patient counseling; steps involved in pati...
 
KARNAADA.pptx made by - saransh dwivedi ( SD ) - SHALAKYA TANTRA - ENT - 4...
KARNAADA.pptx  made by -  saransh dwivedi ( SD ) -  SHALAKYA TANTRA - ENT - 4...KARNAADA.pptx  made by -  saransh dwivedi ( SD ) -  SHALAKYA TANTRA - ENT - 4...
KARNAADA.pptx made by - saransh dwivedi ( SD ) - SHALAKYA TANTRA - ENT - 4...
 
Over the counter (OTC)- Sale, rational use.pptx
Over the counter (OTC)- Sale, rational use.pptxOver the counter (OTC)- Sale, rational use.pptx
Over the counter (OTC)- Sale, rational use.pptx
 
How to Manage Cross-Selling in Odoo 17 Sales
How to Manage Cross-Selling in Odoo 17 SalesHow to Manage Cross-Selling in Odoo 17 Sales
How to Manage Cross-Selling in Odoo 17 Sales
 
In - Vivo and In - Vitro Correlation.pptx
In - Vivo and In - Vitro Correlation.pptxIn - Vivo and In - Vitro Correlation.pptx
In - Vivo and In - Vitro Correlation.pptx
 
Drug Information Services- DIC and Sources.
Drug Information Services- DIC and Sources.Drug Information Services- DIC and Sources.
Drug Information Services- DIC and Sources.
 
HED Office Sohayok Exam Question Solution 2023.pdf
HED Office Sohayok Exam Question Solution 2023.pdfHED Office Sohayok Exam Question Solution 2023.pdf
HED Office Sohayok Exam Question Solution 2023.pdf
 
DUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRA
DUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRADUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRA
DUST OF SNOW_BY ROBERT FROST_EDITED BY_ TANMOY MISHRA
 
How to Create a Toggle Button in Odoo 17
How to Create a Toggle Button in Odoo 17How to Create a Toggle Button in Odoo 17
How to Create a Toggle Button in Odoo 17
 
Protein Structure - threading Protein modelling pptx
Protein Structure - threading Protein modelling pptxProtein Structure - threading Protein modelling pptx
Protein Structure - threading Protein modelling pptx
 

Bioadhesive drug delivery system

  • 1. By,  Dr. Shreeraj Shah  Associate Professor,  Dept. of Pharmaceutical Technology  L.J. Institute of Pharmacy, Ahmedabad
  • 2. Bioadhesion may be defined as the state in which two materials, at least one of which is biological in nature, are held together for extended periods of time by interfacial forces.  The rationale being that the formulation will be ‘held’ on a biological surface for localized drug delivery.  The API will be released close to the site of action with a consequent enhancement of bioavailability.  It is a phenomenon of interfacial molecular attractive forces amongst the surfaces of the biological substrate and the natural or synthetic polymers, which allows the polymer to adhere to the biological surface for an extended period of time  For the purpose of drug delivery system Drug carrier system  adhere to biological tissue  increase concentration gradient at the absorption site  increase the bioavailability.  Also used for • local target to the mucosal surface • reduce the side effect
  • 3.  Mucoadhesion is commonly defined as the adhesion between two materials, at least one of which is a mucosal surface.  Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for improved therapeutic outcome.
  • 4.  Bioadhesion is defined as an ability of a material to adhere to a biological tissue for an extended period of time.  In the case of polymer attached to the mucin layer of a mucosal tissue, the term “mucoadhesion” is used.
  • 5. The ideal characteristics of a Bio/Mucoadhesive approach include: The rapid adherence to the mucosal layer without any change in the physical property of the delivery matrix, minimum interference to the release of the active agent, biodegradable without producing any toxic byproducts,  enhance the penetration of the active agent (if the active agent is meant to be absorbed from the delivery site)
  • 6. The formulation stays longer at the delivery site improving API bioavailability using lower API concentrations for disease treatment  The use of specific bioadhesive molecules allows for possible targeting of particular sites or tissues  Increased residence time combined with controlled API release may lead to lower administration frequency  The avoidance of first-pass metabolism  Dose-related side effects may be reduced due to API localization at the disease site  These dosage forms facilitate intimate contact of the formulation with the underlying absorption surface. This allows modification of tissue permeability for absorption of macromolecules ,such as peptides and proteins. Inclusion of penetration enhancers such as Sodium glycocholate, Sodium taurocholate and L-lysophosphotidyl choline and protease inhibitors in the mucoadhesive dosage forms resulted in better absorption of peptides and proteins.
  • 7. Medications administered orally do not enter the blood stream immediately after passage through the buccal mucosa. Instead they have to be swallowed and then have to pass through a portion of the GIT before being absorbed. So the action is not very rapid in the GIT as compared when the drug is administered through buccal route.  Certain drugs when ingested undergo drug destruction, there are several drugs which are potentially in this category. Many drugs affect liver metabolism and also cause destruction via first pass metabolism of other drugs.  Oral ingestions results in more exposure of a drug to the GI tract. One of the side effects of many antibiotics is the destruction of normal GI flora resulting in diarrhea and overgrowth with dangerous organisms such as C. difficile.  The absorption of mucoadhesive drugs is adversely affected by the presence of food. Tetracyclines, in particular, complicates the administration of this class of antibiotics via the oral route.
  • 8. Mucoadhesive Inner layers called mucosa Inner epithelial Cell lining Covered with viscoelastic fluid.  It is secreted by Goblet cells lining the epithelia or by special exocrine glands with mucus cells composed of water and mucin (an anionic polyelectrolyte).  Other components include proteins, lipids, electrolytes and mucopolysaccharides  Thickness varies from ≈40–50 μm to ≈300 μm
  • 10. General composition of mucus : Water……………………….95% Glycoprotiens and lipids….0.5-5% Mineral salts……………….1% Free proteins………………0.5-1%  These units contain an average of about 8-10 monosaccharide residues of five different types. They are: a) L-fucose b) D-galactose c) N-acetyl-D-glucosamine d) N-acetyl-D-galactosamine e) Sialic acid
  • 11. Complex-high molecular weight macromolecule consisting of a polypeptide (protein) backbone to which carbohydrate side chains are attached. Generic structure of mucin monomer
  • 12. Mucus forms flexible, threadlike strands that are internally cross linked by disulphide bond. Disulphide bond present in mucus The mucus layer which covers the epithelial surface has various roles: • Protective • Barrier • Adhesion • Lubrication
  • 13. MUCUS MEMBRANE STRUCTURE STRUCTURE OF MUCIN
  • 14. The mechanisms responsible in the formation of mucoadhesive bonds are not fully known, however most research has described mucoadhesive bond formation as a three step process. Step 1 : Wetting and swelling of polymer (the contact stage) Step 2 : Interpenetration between the polymer chains and the mucosal membrane Step 3 : Formation of chemical bonds between the entangled chains (both known as consolidation stage)
  • 15. Step 1 The wetting and swelling step occurs when the polymer spreads over the surface of the biological substrate or mucosal membrane in order to develop an intimate contact with the substrate. This can be readily achieved for example by placing a mucoadhesive formulation such as a tablet or paste within the oral cavity or vagina. Swelling of polymers occur because the components within the polymers have an affinity for water.
  • 16. Step 2 The surface of mucosal membranes are composed of high molecular weight polymers known as glycoproteins. In step 2 of the mucoadhesive bond formation, the mucoadhesive polymer chains and the mucosal polymer chains intermingle and entangle to form semi permeable adhesive bonds. The strength of these bonds depends on the degree of penetration between the two polymer groups. In order to form strong adhesive bonds, one polymer group must be soluble in the other and both polymer types must be of similar chemical structure.
  • 17. Step 3 This step involves the formation of weak chemical bonds between the entangled polymer chains. The types of bonding formed between the chains include primary bonds such as covalent bonds and weaker secondary interactions such as van der Waals Interactions and hydrogen bonds. Both primary and secondary bonds are exploited in the manufacture of mucoadhesive formulations in which strong adhesions between polymers are formed.
  • 18.  The Theories include :- (1) The electronic theory. (2) The wetting theory. (3) The adsorption theory. (4) The diffusion theory. (5)The Fracture theory (6) The mechanical theory. (7) The cohesive theory.  The phenomena of bioadhesion occurs by a complex mechanism. There are seven theories have been proposed till date
  • 19. 1) The Electronic theory  Electronic theory is based on the premise that both mucoadhesive and biological materials possess opposing electrical charges. Thus, when both materials come into contact, they transfer electrons leading to the building of a double electronic layer at the interface, where the attractive forces within this electronic double layer determines the mucoadhesive strength 2) The wetting theory  The wetting theory applies to liquid systems which present affinity to the surface in order to spread over it. This affinity can be found by using measuring techniques such as the contact angle. The general rule states that the lower the contact angle then the greater the affinity. The contact angle should be equal or close to zero to provide adequate spreadability
  • 21. 3) The Adsorption theory  According to the adsorption theory, the mucoadhesive device adheres to the mucus by secondary chemical interactions, such as in van der Waals and hydrogen bonds, electrostatic attraction or hydrophobic interactions. For example, hydrogen bonds are the prevalent interfacial forces in polymers containing carboxyl groups.  Such forces have been considered the most important in the adhesive interaction phenomenon because, although they are individually weak, a great number of interactions can result in an intense global adhesion
  • 22. 4) The diffusion theory  Diffusion theory describes the interpenetration of both polymer and mucin chains to a sufficient depth to create a semi-permanent adhesive bond. It is believed that the adhesion force increases with the degree of penetration of the polymer chains  This penetration rate depends on the diffusion coefficient, flexibility and nature of the mucoadhesive chains, mobility and contact time.  According to the literature, the depth of interpenetration required to produce an efficient bioadhesive bond lies in the range 0.2-0.5 μm
  • 23. 5) The Fracture theory  This theory attempts to relate the difficulty of separation of two surfaces after adhesion  It analyzes the force required to separate two surfaces after adhesion Adhesion Strength = (E ԑ/L )1/2 E =Young’s modulus of elasticity ԑ = Fracture energy L = Critical crack length when two surfaces are separated
  • 24. 6) The mechanical theory  Mechanical theory considers adhesion to be due to the filling of the irregularities on a rough surface by a mucoadhesive liquid. Moreover, such roughness increases the interfacial area available to interactions thereby aiding dissipating energy and can be considered the most important phenomenon of the process 7) The cohesive theory  It proposes that the phenomena of bioadhesion are mainly due to the intermolecular interactions amongst like-molecules.
  • 25. Polymer related factors: Molecular weight Concentration of active polymer Flexibility of polymer chains Hydrogen bonding capacity Presence of functional group Spatial conformation Cross linking density Charge on polymer Hydration Hydrophilicity  Environment related factors : pH of polymer – substrate interface Applied strength Initial contact time Swelling  Physiological factors: mucin trun over
  • 26. POLYMER RELATED FACTORS:- 1) Molecular weight  Bioadhesion is maximum at certain molecular weight.  Low molecular weight  interpenetration is more  High molecular weight  entanglement is more  Bioadhesive force of polymers is increase up to molecular weight 10000, beyond which there is no further gain. 2) Concentration of active polymer  In high concentration coiled molecules of polymer become solvent poor and chains available for bioadhesion are less.  In low concentration bioadhesion of polymer also decreases.
  • 27. 3) Degree of hydration  Depending on the degree of hydration adhesive properties are different. It is maximum at a certain degree of hydration.  High degree of hydration  formation of slippery, non- adhesive mucilage due to large amount of water leads to loss of adhesiveness. 4) Charge on polymer  Mucosal surface is negatively charged. So positively charged polymer might facilitate the mucoadhesive process.  Chitosan have bioadhesion due to electrostatic attraction between positively charged D- glucosamine residue of chitosan and negatively charged sialic acid residues.
  • 28. 5) Presence of functional group  Due to immobilization of thiol groups on polymers like chitosan & polyacrylic acid their permeation enhancement, enzyme inhibitory & mucoadhesive properties are improved.  The immobilization of thiol groups on microparticles improves mucoadhesive properties. 6) Spatial conformation  Besides molecular weight or chain length, spatial conformation of a polymer is also important. Despite a high molecular weight of 19,50,0000 for dextrans, they have adhesive strength similar to that of polyethylene glycol (PEG), with a molecular weight of 2,00,000. The helical conformation of dextran may shield many adhesively active groups, primarily responsible for adhesion, unlike PEG polymers, which have a linear conformation.
  • 29. ENVIRONMENT RELATED FACTORS:- (1) pH • pH influences the charge on the surface of both mucus and the polymers. • Mucus will have a different charge density depending on the pH because of the difference in the dissociation of the functional groups on the carbohydrate moiety and amino acids of the polypeptide backbone. • Polyacrylic acid polymers  degree of hydration increase upto pH 4 to 5  slightly increase at pH 6 to 7  decreasing at more alkaline pH. (2) Applied strength • To place a solid bioadhesive system, it is necessary to apply a defined strength. The adhesion strength increases with the applied strength or with the duration of its application, up to an optimum level.
  • 30. (3) Initial contact time  The initial contact time between the mucoadhesives and the mucus layer determines the extent of swelling and the interpenetration of the polymer chains.  The mucoadhesive strength increases as the initial contact time increases. (4) Swelling  Interpenetration of chains is easier when polymer chains are disentangled and free of interactions.  When swelling is too great, a decrease in the bioadhesion occurs, such phenomena must not occur too early, in order to lead to a sufficient time for action of the bioadhesive system.
  • 31. PHYSIOLOGICAL FACTORS:- (1) Mucin turnover  The natural turnover of the mucin molecules from the mucus layer is important for at least two reasons-  The mucin turn over is expected to limit the residence time of mucoadhesive dosage form on the mucus layer.  Mucin turnover results in substantial amount of soluble mucin molecules. These mucin molecules interact with mucoadhesive dosage form before they have a chance to interact with the mucus layer. (2) Disease states  The physiological properties of the mucus are known to change during disease conditions such as the common cold, gastric ulcers etc. The exact structural changes taking place in mucus under these conditions are not yet clearly understood.
  • 32.  They are water soluble and water insoluble polymers which are swellable networks joined by cross linking agents.  Characteristic of ideal polymer  Degradation products should be non toxic and non absorbable from GIT  Good spreadability, wetting, swelling, solubility and biodegradability properties  Optimum molecular weight  Non irritant to mucous membrane  Form a strong non covalent bond with mucin epithelial cell surfaces
  • 33.  Adhere quickly to moist tissue  Allow easy incorporation of the drug  Not decompose on storage or during shelf life of dosage form  Should possess site specificity  Cost effective  Should approved by regulatory authorities
  • 34. According to source Natural and modified natural Synthetic Agaros Carbopol Chitosan Polycarbophil Gelatin Polyacrylic acid Hyaluronic acid Polyacrylates Carrageenan Methacrylic acid Pectin Poly Vinyl Alcohol Sodium alginate Poly Vinyl Pyrollidine Carboxy Methyl Cellulose Ethylhexaacrylate Thiolated CMC Thiolated polymer, etc. Sodium CMC HEC HPC HPMC Methylhydroxyethylcellulose, etc.
  • 35. According to water solubility Water soluble Water insoluble CMC, Thiolated CMC, Sodium Carbopol,Polycarbophil, CMC, HEC, HPC,HPMC, MC, Polyacrylic acid, Polyacrylates HPMC,PVA,PVP, etc. Methacrylic acid, PEG, etc. According to charge Cationic and Anionic Uncharged Aminodextran, Chitosan, Hydroxyethylated starch, Chitosan-EDTA, Carbopol HPC, PEG Polycarbophil, Sodium alginate, PVA, PVP, etc. Pectin, Sodium CMC, CMC, etc.
  • 36. Route/site Bioadhesive formulation Oral cavity (Buccal Tablet, Patch, Gel, Ointment, and Sublingual) Chewing gum, Hollow fibers Nasal Gel, Microspheres, Dry powders Ocular Insert, gel Gastro intestinal Gel, Tablet, Microspheres, Capsule, Hollow fibers Skin/Transdermal Patch, Liposomes Vaginal Gel, Microspheres, Tablet Rectal Gel
  • 37.  Bioadhesive tablets are immobilized drug delivery systems  Formulated as monolithic, partially coated or multilayered matrices  Formulation ingredients 1) API 6) Sweetening agent 2) Mucoadhesive polymer 7) Flavoring agent 3) Permeation enhancer 8) Coloring agent 4) Diluent 9) Buffering agent 5) Lubricant 10) Backing layer polymers
  • 39. Small surface of contact with mucosa  Lack of physical flexibility  Difficult to obtain high release rate, which is required for some drugs  The extent and frequency may cause irritation to mucosa
  • 40. 1)Weight variation 2) Thickness 3) Hardness 4) Friability 5) Drug content 6) Surface pH 7) In vitro drug release 8) In vitro drug permeation 9) Swelling study 10) Measurement of residence time / retention time 11) Adhesive strength determination
  • 41. Measurement of residence time / retention time  Provides quantitative information on mucoadhesive properties.  The GI transit time of many mucoadhesives have been examined using radioisotopes . e.g. 51Cr and the time dependent distribution of the radioactivity in the GIT is measured.  Esophageal bioadhesive property porcine oesophageal tissue is used.  tissue is washed at a rate of 1ml/min with simulate saliva flow.  1.5 mL of formulation was mixed with ~0.2 MBq Tc99m as a radioactive substance. Eluate is collected upto 30 min. fig : In-vitro apparatus used to measure the residence time to perticular tissue. 41
  • 42. Measurement of mucoadhesive strength Three different types of stress, tensile, shear and peel stress are measured A) Tensile strength
  • 43. B) Shear and Peel strength C) Thumb test The adhesiveness is qualitatively measured by the difficulty of pulling the thumb from the adhesive as a function of the pressure and the contact time. It provides useful information on mucoadhesive potential
  • 45. Dissolution of Buccal tablet:- fig : Mumtaz and Chang model for the dissolution of the buccal tablet.  From the inlet dissolution medium is poured and from outlet it is collected and assayed.   45
  • 46. Gels includes bioadhesive gels and in situ forming gels  Bioadhesive gels  These gels highly viscous semisolids prepared by using mucoadhesive polymers  Formulated for various sites like buccal, nasal, vaginal, rectal,etc
  • 47.  Formulation ingredients of bioadhesive gel 1) Active pharmaceutical ingredient 2) Mucoadhesive polymer 3) Permeation enhancer 4) Preservative 5) Solvent
  • 48. In situ gels are in solution form and formed gels upon administration to particular site due to phase transition in environment of that site  Gel formation is due to various mechanisms includes,  Thermal change  pH change  change in electrolyte composition  combination of any 2 mechanisms
  • 49. Thermo sensitive gel forming system Thermo sensitive polymer systems are formed from aqueous polymer solutions with temperature changes Thermo sensitive polymers are copolymers of N- isopropylacrylamide (PNiPAAM), polaxamer, etc. pH sensitive gel forming system pH sensitive gel forming systems, which swell or shrink in response to changes in the pH Carbopol (polyacrylic acid) is mostly used as pH sensitive polymer
  • 50.  Ion sensitive gel forming system  Ion sensitive gel forming system is new type of gel, in which solution of polymer containing drug triggered to gel form when contact with specific ion at specific site  Ion sensitive polymer includes sodium alginate, gellan gum, xyloglucan, carrageenan  In situ gels formulate for various sites including nasal, ophthalmic, oral, vaginal, rectal
  • 51. 1) Drug content 2) Viscosity 3) pH 4) In vitro drug release 5)Adhesion properties: Adhesive strength is measured as described in tablets and the other methods are, A)Membrane viscosity  The interaction between polymers and cell membranes was examined by labeling the cell membranes with fluorescent probes
  • 52.  The lipid bilayer and proteins of cell membranes were labeled with pyrene and fluorescein isothiocyanate  The fluorescence spectrum of pyrene and the fluorescence depolarization of fluorescein isothiocyanate were used to examine the change in membrane viscosity after interaction with polymer  It was assumed in this study that affinity of polymers to cell membranes is linearly related to the increase in membrane viscosity
  • 53. B) Electrical conductance  The adhesion of orabase, carbopol, guar gum, and methyl cellulose to artificial biomembrane in artificial saliva was studied by using a modified rotational viscometer capable of measuring electrical conductance  In presence of adhesive material the conductance was comparatively low. As the adhesive was removed the value increased to final corresponding to conductance of saliva, which indicate the absence of adhesion
  • 54.  Patches are designed for buccal delivery and transdermal delivery of drugs  Buccal patches  Designed either for unidirectional release or bidirectional release  Use of impermeable backing layer will maximize the drug concentration gradient and prolong adhesion because the system is protected from saliva  Typically size of such polymeric patches would be 1-3 cm 2 but may have dimensions as large as 10-15 cm2 depending on the site of administration
  • 55. Patch contains mucoadhesive polymer and supportive material Matrix system Reservoir system
  • 56.  Formulation ingredients of Buccal patch 1) API 2) Mucoadhesive polymer 3) Supporting material 4) Plasticizer  Evaluation of Buccal patch 1) Thickness uniformity 2) Folding endurance 3) Uniformity of weight 4) Drug content uniformity 5) Swelling study 6) Surface pH 7) In vitro release study 8) Adhesive strength
  • 57.  Transdermal patches  Transdermal patch is a medicated adhesive placed on the skin to deliver a specific dose of medication through the skin and into bloodstream  Formulation is same as buccal patches  Evaluation of Transdermal patches 1) Thickness uniformity 2) Moisture content 3) Uniformity of weight 4) Drug content uniformity 5) Flatness study 6) Surface pH 7) In vitro release study 8) Adhesive strength
  • 58. Mucoadhesion measurement by Modified balance method
  • 59. Chewing gums are mobile drug delivery systems  The main target mucosa for drug absorption is sublingual mucosa  Drug release is generally rapid but not as immediate as in case of fast dissolving tablets  Commercially available medicated chewing gums are currently available for pain relief, smoking cessation, travel illness, and freshening of breath  Medicated chewing gum offers advantages in comparison to conventional oral mucosal and oral dosage forms both for (a) local treatment of mouth diseases and (b) systemic effect after absorption through the buccal and sublingual mucosa or from the gastrointestinal tract
  • 60. Components of chewing gum Component Concentration (%) Drug Max. approximately 50 Gum base 20–40 Bulk sweeteners 30-75 Softeners 0-10 Flavoring agents 1-5 Coloring agents ˂1
  • 61. Manufacturing process of chewing gum  The most common method comprises mixing the gum base with the other ingredients in a mixer with Z formed blades. The gum base can either be added in a solid form and softened through heating from the jacket of the mixer or from the frictional heat generated during the mixing process, or it can be added in a melted form.  Chewing gum can also be manufactured by compression of powders or granulates on a conventional tablet machine (compression technique).
  • 62. The release into saliva and disappears rapidly from the oral cavity because of involuntary swallowing  The concentration drug in the oral cavity always tends to decrease as a result of salivary dilution  The drug is not protected from the environment found in oral cavity  Administration of such dosage form is restricted to short time periods because the delivery system in the oral cavity causes disturbance in drinking, eating and speaking
  • 63.  Films are used for buccal bioadhesive drug delivery  Both degradable and non-degradable forms of films have been developed  The major method of polymeric film manufacture is the solvent evaporation process  Formulation ingredients 1) API 2) Mucoadhesive polymer 3) Plasticizer
  • 64.  Evaluation of film 1) Weight uniformity 2) Thickness 3) Swelling study 4) folding endurance 5) Drug content uniformity 6) Surface pH 7) In vitro drug release 8) Mucoadhesion study
  • 65. Solid ophthalmic delivery devices (inserts) are thin disks or small cylinders made with appropriate polymeric materials and fitting into the lower or upper conjuctival sac  Their long persistence in the perocular area can result in a greater drug bioavailability with respect to liquid and semisolid formulations  Mucoadhesive polymers can be profitably used as constituents of inserts to achieve prolonged contact with the conjuctival tissue
  • 66. Alternative approach for chewing gum formulations  The design of micro porous hollow fiber of polysulphone intended for the delivery of histerelin, a LHRH agonist was reported (Burnside et al.)  This fiber is intended to be placed in the buccal cavity for oral mucosal drug delivery  The fiber may also prepare for periodontal application
  • 67. Multiparticulate system includes microspheres, liposomes and nanoparticles Microspheres  Bioadhesive microspheres include micro particles and microcapsules(size 1–1000µm in diameter)  They have the potential to be used for targeted and controlled release drug delivery; but coupling of bioadhesive properties to microspheres has additional advantages,  Efficient absorption and enhanced bioavailability of the drugs due to a high surface to volume ratio  A much more intimate contact with the mucus layer  Specific targeting of drugs to the absorption site
  • 68.  Bioadhesive microspheres can be tailored to adhere to any mucosal tissue including those found in eye, nasal cavity, urinary and gastrointestinal tract, thus offering the possibilities of localized as well as systemic controlled release of drugs  Their formulation contains API and mucoadhesive polymer  Liposomes  Liposomes are coated with mucoadhesive polymers and remain for longer period of time and improved the drug therapy  Ocular route is widely used for mucoadhesive liposomal preparation  Nanoparticles  Nanoparticles prepared for mucoadhesive drug delivery by either consisting entirely of a bioadhesive polymer or having an outer coating of it
  • 69.  Evaluation of multiparticulate system 1) Drug entrapment efficiency 2) Particle size analysis 3) In vitro release study 4) Mucoadhesion study  Mucoadhesion study In microspheres adhesion number is determined  The adhesion number (Na) is, Na = (N/No)*100 Where, No = total no. of applied particles N = no. of particles attached to the substrate  Two methods for measurement A)Falling liquid film method B) Mucin gold staining
  • 70. A)Falling liquid film method The adhesion of particles to this surface is measured by passing the particle suspension over the surface and by comparing the fraction of particles adhered to the tissue
  • 71. B) Mucin gold staining  In this technique, colloid gold particles, which are red in solution, are stabilized by mucin molecules  The interaction between mucin and adhesive particles is monitored by appearance of red color on surface.
  • 72. EVALUATION OF BDDS  IN VITRO / EX VIVO METHODS a. Methods based on measurement of tensile strength. b. Methods based on measurement of shear strength. OTHER IN VITRO METHODS c. Adhesion weight method d. Fluorescent probe method e. Flow channel method f. Falling liquid film method g. Colloidal gold staining method h. Mechanical spectroscopic method I. Thumb test j. Viscometric method k. Adhesion number
  • 73. IN VIVO METHODS a. Use of radio isotopes b. Use of gamma scintigraphy In vivo evaluation methods  In vivo methods used for evaluation are based on administration of polymers to a laboratory animal and tracking their transit through the GI system.  Administration methods include forced oral gavage, surgical stomach implantation and infusion through a loop placed in situ in the small intestine. Tracking generally followed with the help of X-ray studies, radio opaque markers and radioactive elements etc.  For e.g. X- ray studies for monitoring GI transit time for bioadhesive tablet made of BaSO4 and radiolabelled microspheres and nanoparticles. 73
  • 74. Ocular (Eye)  Nasal cavity  Oral (Buccal and Sublingual)  Skin/Transdermal  Gastro-intestinal and Colorectal (Colon+ Rectum)  Vaginal
  • 75. The eye is one of the most important and complex organs of the body, because of its complicated anatomy many things can go wrong with the eye.  Topical drug delivery systems to the eye can be very difficult to achieve because the eye has several protective mechanisms in place to get rid of foreign substances.  An effective ocular drug delivery system must be easy to use, comfortable to the patient and maintain substantial concentrations of the drug in the eye to produce therapeutic effects.  Problems associated with eye include conjunctivitis, Glaucoma and dry eye.
  • 76. Ocular Bioadhesive Formulations  GelTears® and Viscotears® Liquid gel eye drops are used for dry eye conditions and contain carbomer 980 (polyacrylic acid). Carbomers lubricate the eye by clinging to the surface of the eye. This can help reduce the frequency of their application into the eye.  Pilogel® is an eye gel used in the treatment of glaucoma. It contains the high molecular weight polymer polyacrylic acid. The polymer increases the viscosity of the gel which provides a prolonged retention of the gel in the eye.
  • 77. Drugs such as antihistamines and steroids are administered as nasal drops or nasal sprays to treat conditions affecting the nose. However nasal mucociliary clearance affects the retention and therefore the effects of the drugs in the nose.  The effects of bioadhesive polymers on mucociliary clearance was examined by Zhou and Donovan (1996).  Methylcellulose exhibited the most reduction in mucociliary clearance whilst Carbopol 934P showed the least reduction in mucociliary clearance in the rats used.
  • 78. Bioadhesive formulations for Nasal cavity  Rhinocort® Nasal spray is a powdered mixture of the steroid Beclomethasone dipropionate(50μg) and 30mg of Hydroxypropyl cellulose(HPC).  Used for patients suffering from nasal allergy.  The powder sticks to and swells on the cells lining the nose and remains there for about 6 hrs.  Beconase® Nasal spray is used to treat nasal inflammation and nasal allergies associated with hayfever.  It contains the active ingredient Beclometasone dipropionate and the bioadhesive polymers carboxymethyl cellulose and microcrystalline cellulose.  Nasacort® Nasal spray is used to treat allergies that result in inflammation of the nose. The active ingredient in this product is Triamcinolone acetonide as well as the bioadhesive polymer microcrystalline cellulose. The polymer swells in the presence of water and is able to spread across the nasal mucosa thus helping the distribution of the drug over the mucosal surface.
  • 80. The oral cavity or the mouth comprises of the cheeks, teeth and the tongue.  It is an entrance of the digestive system and plays many important functions which include chewing, speaking and tasting.  Some of these functions are impaired by diseases such as ulcers, microbial infections and inflammation. Examples of products  Corlan®: Corlan pellets are used in the treatment of mouth ulcers to reduce the pain, swelling and inflammation associated with mouth ulcers.  The active ingredient of the pellet is Hydrocortisone succinate. It also contains the bioadhesive polymer Acacia which helps prolong the effect of the drug in the oral cavity.
  • 81. The Buccal Mucosa  Buccastem® is a drug used in the treatment of nausea, vomiting and vertigo. It contains the bioadhesive agents Polyvinylpyrrolidone and Xanthan gum.  Suscard® is a buccal tablet used in the treatment of angina. It contains the bioadhesive agent Hydroxypropyl methylcellulose (HPMC). The sublingual mucosa  Drugs administered via the sublingual route are formulated as tablets, powders, solutions or aerosol sprays.  Examples of sublingual products include Glyceryl Trinitrate (GTN) aerosol spray and tablet which is administered under the tongue for the prophylactic treatment of angina.
  • 82.  The skin is the outer covering of the body and consists of different layers. It performs several functions which include:  Protecting the body from injury and invasion by pathogens  Preventing the body from becoming dehydrated  Regulating body temperature  Production of Vitamin D Topical Bioadhesive Formulations  The drug delivery systems used in this case are required to adhere to the skin for the purpose of:  Collecting body fluids  Protecting the skin  Providing local or systemic drug delivery
  • 83. Transdermal Bioadhesive formulations  Voltarol Emulgel: This is a gel which provides a local relief from pain and inflammation in the tendons, muscles and joints.  It contains the bioadhesive polymer carbomer which aids the absorption of the active drug by spreading it into the affected area.  Feldene: This gel is used in the treatment of conditions which are characterised by pain, inflammation and stiffness.  The active ingredient in this formulation is piroxicam but the gel also contains two bioadhesive agents to increase its retention at the absorption site. These agents are Carbopol 980 and hydroxyethyl cellulose.
  • 84. The rectum is the terminal or end portion of the gastrointestinal tract. It is an important route of administration for drugs that have severe gastrointestinal side effects.  This route is also suitable for patients who cannot take medicines via the oral route such as unconscious patients and infants.  The drugs absorbed from the rectum can escape breakdown by hepatic enzymes. For this reason mucoadhesive suppositories have been developed for the local treatment of diseases such as haemorrhoids and rectal cancer.
  • 85. Rectal Bioadhesive Formulations  Anacal® is a rectal ointment used to relieve the symptoms associated with haemorrhoids. It contains the bioadhesive agent polyethylene high polymer 1500.  Germoloids® is a rectal ointment used to relief the pain, swelling, itchiness and irritation associated with haemorrhoids. It contains the polymer propylene glycol.
  • 86.  The vagina is the lower part of the female reproductive tract.  It is a muscular tube lined with mucous membrane which is covered with a layer of stratified squamous epithelium with an underlying layer of connective tissue (lamina propria) Common conditions affecting the vagina  The epithelium of the vagina contains glycogen, which is broken down enzymes and bacteria into acids such as lactic acid. This maintains a low vaginal pH which is normally between 4 and 5.  Such a pH is desirable because it makes the vagina inhospitable to pathogens.  Decreased levels of glycogen in the vagina leads to an increase in vaginal pH and makes the vagina more susceptible to infection such as Vaginitis, Bacterial vaginosis, Candidiasis (Thrush), Trichomoniasis etc..
  • 87. Vaginal bioadhesive formulations  The intravaginal route has been used to deliver contraceptives as well as anti-infective agents such as antifungal drugs to exert a local effect.  Agents targeted for the vaginal route have been formulated into various dosage forms including creams, gels and vaginal tablets.  Bioadhesive polymers are incorporated into vaginal formulations to aid the adhering of the dosage form to its target site.  Polymers also increase the retention of the active drug in the vagina and also optimise the spread of the formulation over the vaginal epithelium.
  • 88. S-DBMP-T(Slowly Disintegrating Buccal Mucoadhesive Plain-Tablet)  BCTS (Buccal Covered-Tablet System)  VagiSiteTM Bioadhesive Technology
  • 89. Iga et al. developed this system  S-DBMP-T are prepared by incorporating a relatively large amount of hydroxypropylcellulose in a tablet formulation  An example of a typical composition is a tablet composed of 20 mg of drug, 20 mg of hydroxypropylcellulose, 20 mg of carboxymethylcellulose (ECG-505, disintegrating agent), and 60 mg of lactose  The S-DBMP-T technology was originally developed for increasing the bioavailability of oxendolone (a steroidal anti-androgen)
  • 90. To maintain the tablet shape for as long as possible, Iga et al. developed a method to restrict disintegration from the sides of the tablets  The method involved sandwiching a S-DBMP-T tablet between two polyethylene sheets. The upper sheet contained a hole that allowed the tablet to absorb water and disintegrate only through the hole. The lower sheet contained adhesives to allow the delivery system to adhere to the gingiva for a long time.
  • 91. Developed by KV Pharmaceutical Company, St. Louis, Missouri, U.S.A.  The VagiSiteTM technology comprises a high-internal-phase- ratio, water-in-oil emulsion  The internal phase of the emulsion acts as the carrier of the active drug. The drug-laden internal-dispersed phase globules serve a dual purpose for both the sequestering and the controlled release of the active agent, butoconazole nitrate  After introduction of the drug-containing emulsion to a mucosal surface, in this case the vaginal mucosa, a thin bioadhesive film of contiguous drug-laden internal-phase globules forms on the mucosal surface
  • 92. Rathbone MJ et al., Modified Release Drug Delivery Technology, Marcel Dekker, Inc., 2002, 349-81, 801-6  Vyas SP, Khar RK., Controlled Drug Delivery: Concepts and Advances, Vallabh Prakashan, First Edition: 2002, 257-314  Methiowitz E et al., Bioadhesive Drug Delivery System, Marcel Dekker, Inc., 1999, 551-3, 621-31  Andrews GP et al., Mucoadhesive polymeric platforms for controlled drug delivery, European Journal of Pharmaceutics and Biopharmaceutics 71 (2009) 505–18  Salamat-Miller N et al., The use of mucoadhesive polymers in buccal drug delivery, Advanced Drug Delivery Reviews 57 (2005) 1666– 91