This document discusses nanoparticles for drug delivery. It begins with an introduction to nanoparticles and their properties. Some advantages of nanoparticles include reduced dosing frequency and improved drug solubility. Nanoparticles can be classified as nanospheres or nanocapsules. Common preparation methods are polymerization, precipitation and crosslinking. Nanoparticles are evaluated based on size, drug release, yield and stability. Finally, applications include cancer therapy, intracellular targeting and ocular delivery.
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Rahela Eyachmin Laskar's Guide to Nanoparticles
1. PRESENTED BY
RAHELA EYACHMIN LASKAR
M.PHARM
FACULTY OF PHARMACEUTICAL SCIENCE
ASSAM DOWN TOWN UNIVERSITY
UNDER THE GUIDANCE OF
ANANTA CHOUDHURY
ASSOCIATE PROFESSOR
FACULTY OF PHARMACEUTICAL SCIENCE
ASSAM DOWN TOWN UNIVERSITY
2. INTRODUCTION
IDEAL PROPERTIES
ADVANTAGES AND DISADVANTAGES
TYPES OF NANOPARTICLES
METHOD OF PREPARATIONS
EVALUATIONS
APPLICATIONS
CONCLUSION
CONTENT
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3. Nanoparticles are defined as particulate dispersions
or solid particles with a size in the range of 10-1000nm
The drug dissolved, entrapped, encapsulated or
attached to a nanoparticle matrix.
They are composed of synthetic or semi synthetic
polymers carrying drugs.
After the administration, nanoparticles are mainly
taken by Reticulo Endothelial System (RES).
INTRODUCTION
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4. It should be biochemical inert and non toxic.
It should be stable both physically and chemically in In
-vivo & In- vitro conditions.
Controllable & Predicate rate of drug release.
Carriers used must be biodegradable or readily
eliminated from the body without any problem.
The preparation of the delivery system should be easy
or reasonable.
IDEAL PROPERTIES OF
NANOPARTICLES
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5. Reduction in the frequency of the dosages taken by
the patient.
More uniform effect of the drug .
Nanoparticle enhance the aqueous solubility of poorly
soluble drug, which improves bioavailability of drug.
Avoids hepatic first pass metabolism.
Nanoparticles can be administer by various routes
including oral, nasal, parenteral, intra-ocular etc.
ADVANTAGES
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6. Due to small particle size nanoparticles overcome
resistance by physiological barriers in the body easily
penetrates to cell walls, blood vessels etc.
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ADVANTAGES
7. High cost
Small size & large surface area can lead
to particle aggregation.
Physical handling is difficult
Requires skills to manufacture
DISADVANTAGES
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8. NANOSPHERES: Nano spheres are solid core spherical
particulates, which contain drug embedded within the
matrix or adsorbed onto the surface.(Matrix type)
NANOCAPSULES: Nano capsules are vesicular system in
which drug is essentially encapsulated within the central
core surrounded by a polymeric sheath.(Reservoir type).
TYPES OF NANOPARTICLES
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9. Zero dimension – length , breadth and height are
confined at single point ( for e.g. Nano dots , Nano
particles)
One Dimension _ It has only one parameter length or
breadth ( for e.g. , nanowires and nanotubes)
Two dimensions – It has only two parameter either
length or breadth or height ( e.g. very thin surface
coatings).
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BASED ON DIMENSIONS
10. Based on Dimensions
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Three Dimensions - It has all the parameter of length ,
breadth and height. ( for e.g. crystals).
12. 1) CROSS LINKING OF AMPHIPHILIC
MACROMOLECULES
Nanoparticles can be prepared from amphiphilic
macromolecules, proteins and polysaccharides (which
have affinity for aqueous and lipid solvents).
Techniques involves – Aggregation of amphiphiles
further stabilization either by heat denaturation or
chemical cross linking.
PREPARATION OF NANOPARTICLES
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14. A) EMULSION POLYMERIZATION:
Emulsion polymerization is a type of radical
polymerization that usually starts with an emulsion
incorporating water, monomer, and surfactant. The
most common type of emulsion polymerization is an
oil-in-water emulsion, in which droplets of monomer
are emulsified in a continuous phase of water. The
polymerization process can be initiated by different
mechanisms.
2) POLYMERIZATION BASED
METHODS
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15. 15
A) EMULSION POLYMERIZATION
Initiation occurs when a monomer molecule dissolved
in the continuous phase collides with an initiator
molecule that might be an ion or a free radical
Alternatively, the monomer molecule can be
transformed into an initiating radical by high-energy
radiation, including g-radiation, or ultraviolet or
strong visible light. Chain growth starts when initiated
monomer ions or monomer radicals collide with other
monomer molecules according to an anionic
polymerization mechanism.
16. It is a precipitation polymerization in which monomers,
initiators, and colloid stabilizers are dissolved in a solvent
forming initially a homogeneous system that produces
polymer and results in the formation of polymer particles.
The solvent selected as the reaction medium is a good
solvent for the monomer and the initiator, but is a non-
solvent for the polymer.
Nucleation is directly induced in Aq. Monomer solution. So
stabilizer / surfactant is not needed
B) DISPERSION POLYMERIZATION
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17. B) DISPERSION POLYMERIZATION
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Initiation here is achieved by different mechanism,
but mostly it is by irradiating solution with high
energy radiation (g, UV, strong visible light).
Polymerization is initiated by adding a catalyst &
proceeds with nucleation phase followed by growth
phase.
18. It involves step polymerization of two different
monomers, dissolved in two phases respectively,
Continuous and Dispersed phase. Polymerization
reaction takes place at the interfaces of two liquids.
Nanometer-sized hollow polymer particles were
synthesized by employing interfacial cross-linking
reactions as polyaddition and polycondensation or
radical polymerization.
C) INTERFACIAL POLYMERIZATION
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19. 1) Emulsion-Solvent Evaporation Method
Emulsification-solvent evaporation involves two
steps-
The first step requires emulsification of the polymer
solution into an aqueous phase. During the second
step polymer solvent is evaporated, inducing polymer
precipitation as Nano spheres.
3) POLYMER PRECIPITATION
METHOD
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20. 1) Emulsion-Solvent Evaporation Method
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The Nano particles are collected by ultracentrifugation and
washed with distilled water.
21. 2) Double Emulsion and Evaporation Method:
It involves the addition of aqueous drug solutions to
organic polymer solution under vigorous stirring to
form w/o emulsions.
This w/o emulsion is added into second aqueous phase
with continuous stirring to form the w/o/w emulsion.
The emulsion then subjected to solvent removal by
evaporation and nan particles can be isolated by
centrifugation at high speed.
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22. 3) Emulsions- Diffusion Method
Polymer is dissolved in a partially water-miscible solvent
(such as propylene carbonate, benzyl alcohol), and
saturated with water to ensure the initial
thermodynamic equilibrium of both liquids.
Subsequently, the polymer-water saturated solvent
phase is emulsified in an aqueous solution containing
stabilizer, leading to solvent diffusion to the external
phase and the formation of Nano spheres or Nano
capsules, according to the oil-to-polymer ratio.
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24. 4) Salting Out Method
Salting-out is based on the separation of a water
miscible solvent from aqueous solution via a salting-
out effect.
Polymer and drug are initially dissolved in a solvent
which is subsequently emulsified into an aqueous gel
containing the salting out agent (electrolytes, such as
magnesium chloride and calcium chloride, or non-
electrolytes such as sucrose) .
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25. 4) Salting Out Method
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This oil/water emulsion is diluted with a sufficient volume of water
or aqueous solution to enhance the diffusion of solvent into the
aqueous phase, thus inducing the formation of Nano spheres.
26. 5) Solvent Displacement / Precipitation
method:
Polymers, drug, and or lipophilic surfactant are
dissolved in a semi polar water miscible solvent such as
acetone or ethanol. The solution is then poured or
injected into an aqueous solution with or without
presence of surfactant under magnetic stirring. Nano
particles are formed instantaneously by the rapid
solvent diffusion.
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27. 1) Particle size: Particle size distribution and morphology
are the most important parameters of characterization of
nanoparticles. Morphology and size are measured by
electron microscopy.
2) Drug Release: The technique used for this analysis is
classical analytical methods like UV spectroscopy or high
performance liquid chromatography (HPLC) after
ultracentrifugation, ultra filtration, gel filtration, or
centrifugal ultrafiltration. Quantification is performed
with the UV spectroscopy or HPLC.
EVALUATIONS
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28. EVALUATIONS
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3) Yield of Nanoparticles :
The yield of nanoparticles was determined by comparing
the whole weight of nanoparticles formed against the
combined weight of the copolymer and drug.
%yield = Amount of nanoparticles/amount of drug
+ Polymer *100
4) Specific Surface Area :
specific surface area A = 6/Density x diameter of particle
29. EVALUATIONS
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5) Stability of Nanoparticles :
Stability studies of prepared nanoparticles
determined by storing optimized formulation at
4°C ±1°C and 30°C ± 2°C in stability chamber for
90 days. The samples were analyzed after a
time period like at 0, 1, 2, and 3 months for their
drug content, drug release rate (t50%) as well as
any changes in their physical appearance .
30. EVALUATIONS
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6) In-vitro release Study :
In-vitro drug release studies were performed in USP
Type II dissolution apparatus at rotation speed of 50
rpm. The prepared immersed in 900ml of phosphate
buffer solution in a vessel, and temperature was
maintained at 37±0.20°C. Required quantity 5ml of the
medium was withdrawn at specific time periods and the
same volume of dissolution medium was replaced in the
flask to maintain a constant volume.
31. EVALUATIONS
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The withdrawn samples were analyzed using UV
spectrophotometer.
7) STRUCTURE & CRYSTALLINITY:
Many method are used for determination of structure
and crystallinity.
X ray diffraction method are used to determine the
structure and crystallinity.
32. 1) Widely used in case of Cancer Therapy.
2) In intracellular Targeting
3) Used for Prolonged Systemic
Circulation.
4) As a Vaccine Adjuvant.
5) In Case of Ocular delivery.
6) It is used in case of Oligonucleotide
delivery.
APPLICATIONS
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33. Nanoparticle is novel approach for drug delivery
which we can achieve better therapeutic action,
better bioavailability, reduce toxicity. Today
nanoparticles are successfully used in brain targeting,
in cancer therapy etc. nanoparticles gives us an
opportunity to enhance patient compliance for better
therapy.
CONCLUSION
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