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ETHOSOMES AS NOVEL DRUG
DELIVERY SYSTEM
Presented by Ms. SHIKHA Y. SINGH
Under the guidance of Prof. SMITA.S AHER
Kalyani charitable trust’s
Ravidra gambhirrhao Sapkal
Anjaneri, Nashik-422213
CONTENTS
 INTRODUCTION
 ETHOSOMES
 COMPOSITION
 MECHANISM OF ACTION
 ADVANTAGES & DISADVANTAGES
 CHARACTERIZATION
 METHODS OF PREPARATION
 APPLICATION
 CONCLUSION
Presentaionby-ShikhaYSingh
INTRODUCTION
Why we need NDDS?
What is NDDS?
What are the approaches used in
NDDS?
Why TDDS ?
What is vesicular system?
What is Ethosomes?
Presentaionby-ShikhaYSingh
ETHOSOMES
 Ethosomes are “Ethanolic liposomes”.
 Ethosomes were developed by touitou, 1997
 Ethosomes are non-invasive delivery carrier that
enable drugs to reach the deep skin layers and / or
systemic circulation.
 “Soft vesicles” represent novel vesicles carrier for
enhanced delivery through the skin.
 Size of ethosomes vesicles-30nm to few microns.
Presentaionby-ShikhaYSingh
COMPOSITION
It mainly comprises of
Phospholipid- PC, PA, PPG, PS etc
Alcohol- ethanol & isopropyl alcohol
Water
Polyglycol or glycol
Cholesterol
Dye- rodamine & FITC
Vehicle - Carbapol
Presentaionby-ShikhaYSingh
SKIN MECHANISM AFTER DRUG APPLICATION
Presentaionby-ShikhaYSingh
SKIN MECHANISM AFTER DRUG APPLICATION
Presentaionby-ShikhaYSingh
ETHANOL PENETRATION
Presentaionby-ShikhaYSingh
ADVANTAGES:
 Ethosomes enhance permeation of the drug through skin transdermal &
dermal delivery.
 Ethosomes are platforms for the delivery of large & diverse groups of
drugs (peptides, protein molecules)
 Ethosomal systems are much more efficient at delivering a fluorescent
probe (quantum dots) to the skin in terms of quantity & depth.
 Low risk profile- the technology has no large scale drug development
risk, as the toxicological profiles of the ethosomes components are well
documented in the scientific literature.
 High patient compliance- the ethosomes drugs are administered in a
semisolid form (gel/cream), producing high patient compliance. In
contrast, iontophoresis & phonophoresis are relatively complicated to use,
which will affect patient compliance.
 High market attractiveness for products with proprietary technology.
Relatively simple to manufacture with no complicated technical
investments required for the production of ethosomes.
 The ethosomes system is passive, non-passive & available for immediate
commercialization.
Presentaionby-ShikhaYSingh
LIMITATIONS:
 Poor yield.
 In case if shell locking is ineffective then the ethosomes may
coalescence and fall apart on transfer into water.
 Loss of product during transfer form organic to water media.
Future perspective:
 Introduction of ethosomes has intiated new area in transdermal
drug delivery
 Further research in this area will allow better control over drug
release in vivo allowing physicians to make therapy more efficient.
 It offers good opportunity for non-invasive delivery of small-,
medium- & large-sized drug molecules.
 Special emphasis given to skin delivery of proteins & other
macromolecules & for transcutaneous immunization.
Presentaionby-ShikhaYSingh
CHARACTERISATION METHODS:
Vesicle shape- Transmission electron microscopy (TEM), Scanning electron microscopy( SEM)
Entrapment efficiency- Mini column centrifugation method; Fluorescence spectrophotometry
Vesicle size- Dynamic light scattering method
Vesicle Skin interaction study- Confocal laser scanning microscopy; Fluorescence microscopy; TEM.
Eosin-Hematoxylin staining
Phospholipid-ethanol interaction- 31P NMR; Differential scanning calorimeter
Degree of deformability- Extrusion method
Zeta potential- Zeta meter
Turbidity- Nephalometer
In vitro drug release study- Franz diffusion cell with artificial or biological membrane, Dialysis bag diffusion
Drug deposition study- Franz diffusion cell
Stability study- Dynamic light scattering method & TEM
Presentaionby-ShikhaYSingh
METHOD OF PREPARATION
Phospholipid + Drug + Other lipid material
Dissolve in Ethanol in covered vessel with vigorous stirring at room temperature
Add Propylene Glycol at 40°C during stirring
Heat mix upto 30°C
Add water at 30°C
Stir for 5 minuets in covered vessel
Size reduction by sonication or extrusion
Store under refrigeration
COLD METHOD
Presentaionby-ShikhaYSingh
Disperse Phospholipid in
water at 40°C
Ethanol + Propylene Glycol at
40°C
Mix organic phase to aqueous phase
Add drug dissolved in suitable solvent (Water
or Ethanol depending on solubility)
METHOD OF PREPARATION
INJECTION METHOD
CLASSIC DISPERSION METHOD
HOT METHOD
Presentaionby-ShikhaYSingh
APPLICATION
 Delivery of Antiviral drugs
 Topical delivery of DNA
 Transdermal delivery of Hormones.
 Delivery of Anti-parkinsonism agent
 Transcellular Delivery
 Delivery of Anti-Arthritis Drugs
 Delivery of Problematic drug molecules
 Delivery of Antibiotics
 Delivery of Antigen loaded Drugs
 Delivery of NSAIDS
 Widely used in Cosmoceuticals
Presentaionby-ShikhaYSingh
CONCLUSION
 The main limiting factor of transdermal drug
delivery system i.e. epidermal barrier can be
overcome by ethosomes to significant extent.
 The ethosomes more advantages when compared
to transdermal and dermal delivery.
 Ethosomes are the non invasive drug delivery
carriers that enable drugs to reach the deep skin
layers finally delivering to the systemic circulation.
 It delivers large molecules such as peptides,
protein molecules. Simple method for drug delivery
in comparison to Iontophoresis and Phonophoresis
and other complicated methods.
 High patient compliance as it is administrated in
semisolid form (gel or cream) and various
application in Pharmaceutical, Veterinary, Cosmetic
field.
Presentaionby-ShikhaYSingh
ANY QUERIES???
Presentaionby-ShikhaYSingh
Presentaionby-ShikhaYSingh

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ETHOSOMES AS NOVEL DRUG DELIVERY

  • 1. ETHOSOMES AS NOVEL DRUG DELIVERY SYSTEM Presented by Ms. SHIKHA Y. SINGH Under the guidance of Prof. SMITA.S AHER Kalyani charitable trust’s Ravidra gambhirrhao Sapkal Anjaneri, Nashik-422213
  • 2. CONTENTS  INTRODUCTION  ETHOSOMES  COMPOSITION  MECHANISM OF ACTION  ADVANTAGES & DISADVANTAGES  CHARACTERIZATION  METHODS OF PREPARATION  APPLICATION  CONCLUSION Presentaionby-ShikhaYSingh
  • 3. INTRODUCTION Why we need NDDS? What is NDDS? What are the approaches used in NDDS? Why TDDS ? What is vesicular system? What is Ethosomes? Presentaionby-ShikhaYSingh
  • 4. ETHOSOMES  Ethosomes are “Ethanolic liposomes”.  Ethosomes were developed by touitou, 1997  Ethosomes are non-invasive delivery carrier that enable drugs to reach the deep skin layers and / or systemic circulation.  “Soft vesicles” represent novel vesicles carrier for enhanced delivery through the skin.  Size of ethosomes vesicles-30nm to few microns. Presentaionby-ShikhaYSingh
  • 5. COMPOSITION It mainly comprises of Phospholipid- PC, PA, PPG, PS etc Alcohol- ethanol & isopropyl alcohol Water Polyglycol or glycol Cholesterol Dye- rodamine & FITC Vehicle - Carbapol Presentaionby-ShikhaYSingh
  • 6. SKIN MECHANISM AFTER DRUG APPLICATION Presentaionby-ShikhaYSingh
  • 7. SKIN MECHANISM AFTER DRUG APPLICATION Presentaionby-ShikhaYSingh
  • 9. ADVANTAGES:  Ethosomes enhance permeation of the drug through skin transdermal & dermal delivery.  Ethosomes are platforms for the delivery of large & diverse groups of drugs (peptides, protein molecules)  Ethosomal systems are much more efficient at delivering a fluorescent probe (quantum dots) to the skin in terms of quantity & depth.  Low risk profile- the technology has no large scale drug development risk, as the toxicological profiles of the ethosomes components are well documented in the scientific literature.  High patient compliance- the ethosomes drugs are administered in a semisolid form (gel/cream), producing high patient compliance. In contrast, iontophoresis & phonophoresis are relatively complicated to use, which will affect patient compliance.  High market attractiveness for products with proprietary technology. Relatively simple to manufacture with no complicated technical investments required for the production of ethosomes.  The ethosomes system is passive, non-passive & available for immediate commercialization. Presentaionby-ShikhaYSingh
  • 10. LIMITATIONS:  Poor yield.  In case if shell locking is ineffective then the ethosomes may coalescence and fall apart on transfer into water.  Loss of product during transfer form organic to water media. Future perspective:  Introduction of ethosomes has intiated new area in transdermal drug delivery  Further research in this area will allow better control over drug release in vivo allowing physicians to make therapy more efficient.  It offers good opportunity for non-invasive delivery of small-, medium- & large-sized drug molecules.  Special emphasis given to skin delivery of proteins & other macromolecules & for transcutaneous immunization. Presentaionby-ShikhaYSingh
  • 11. CHARACTERISATION METHODS: Vesicle shape- Transmission electron microscopy (TEM), Scanning electron microscopy( SEM) Entrapment efficiency- Mini column centrifugation method; Fluorescence spectrophotometry Vesicle size- Dynamic light scattering method Vesicle Skin interaction study- Confocal laser scanning microscopy; Fluorescence microscopy; TEM. Eosin-Hematoxylin staining Phospholipid-ethanol interaction- 31P NMR; Differential scanning calorimeter Degree of deformability- Extrusion method Zeta potential- Zeta meter Turbidity- Nephalometer In vitro drug release study- Franz diffusion cell with artificial or biological membrane, Dialysis bag diffusion Drug deposition study- Franz diffusion cell Stability study- Dynamic light scattering method & TEM Presentaionby-ShikhaYSingh
  • 12. METHOD OF PREPARATION Phospholipid + Drug + Other lipid material Dissolve in Ethanol in covered vessel with vigorous stirring at room temperature Add Propylene Glycol at 40°C during stirring Heat mix upto 30°C Add water at 30°C Stir for 5 minuets in covered vessel Size reduction by sonication or extrusion Store under refrigeration COLD METHOD Presentaionby-ShikhaYSingh
  • 13. Disperse Phospholipid in water at 40°C Ethanol + Propylene Glycol at 40°C Mix organic phase to aqueous phase Add drug dissolved in suitable solvent (Water or Ethanol depending on solubility) METHOD OF PREPARATION INJECTION METHOD CLASSIC DISPERSION METHOD HOT METHOD Presentaionby-ShikhaYSingh
  • 14. APPLICATION  Delivery of Antiviral drugs  Topical delivery of DNA  Transdermal delivery of Hormones.  Delivery of Anti-parkinsonism agent  Transcellular Delivery  Delivery of Anti-Arthritis Drugs  Delivery of Problematic drug molecules  Delivery of Antibiotics  Delivery of Antigen loaded Drugs  Delivery of NSAIDS  Widely used in Cosmoceuticals Presentaionby-ShikhaYSingh
  • 15. CONCLUSION  The main limiting factor of transdermal drug delivery system i.e. epidermal barrier can be overcome by ethosomes to significant extent.  The ethosomes more advantages when compared to transdermal and dermal delivery.  Ethosomes are the non invasive drug delivery carriers that enable drugs to reach the deep skin layers finally delivering to the systemic circulation.  It delivers large molecules such as peptides, protein molecules. Simple method for drug delivery in comparison to Iontophoresis and Phonophoresis and other complicated methods.  High patient compliance as it is administrated in semisolid form (gel or cream) and various application in Pharmaceutical, Veterinary, Cosmetic field. Presentaionby-ShikhaYSingh