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ETHOSOMES
Presented By:
Saurabh sharma
2nd Semester
Pharmaceutics
School Of Pharmaceutical Sciences
Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Road, Gandhi
Nagar, Bhopal
Session 2018- 2020
1
Flow of Presentation
• Introduction
• Types of ethosomes
• Mechanism of ethosome
• Additives used in ethosome
• Method of preparation
• Characterization of ethosome
• Advantages and limitations
• Summary
Ethosomes are ethanolic liposomes
The ethosomes are vesicular carriers consisting of hydroalcoholic or
hydroglycolic phospholipids in which the concentration of alcohols or their
combination is relatively high.
These are soft, malleable vesicles tailored for enhanced delivery of active
agents.
Ethosomes which are novel permeation-enhancing lipid vesicles
embodying high concentration (20–45%) of ethanol
1
2
3
4
Ethanol effect
 Ethanol acts as a penetration enhancer through the skin. Ethanol
penetrates into intercellular lipids and increases the fluidity of cell
membrane lipids and decrease the density of lipid multilayer of cell
membrane
Ethosomes effect
 Ethosomes permeates very easily inside the deep skin layers, where it
got fused with skin lipids and releases the drugs into deep layer of skin
5
Contd….
6
CLASS EXAMPLES USES
Phospholipid Soya phosphatidylcholine,
Egg phosphatidylcholine,
Dipalmityl phosphatidylcholine,
Distearyl phosphatidylcholine
Vesicles forming component
Polyglycol Propylene glycol, Transcutol As a skin penetration enhancer
Alcohol Ethanol, Isopropyl alcohol For providing the softness for vesicle
membrane, as a penetration enhancer
Cholesterol Cholesterol For providing the stability to vesicle
membrane
Dye Rhodamine-123, Rhodamine
Red, Fluorescene Isothiocynate
(FITC), 6- Carboxy fluorescence
For characterization study
Vehicle Carbopol Ð934 As a gel former
7
Method of
Preparation
Hot method Cold method
8
9
Disperse phospholipid
in water at 40˚C
Ethanol + propylene
glycol at 40˚C
Mix organic phase to
aqueous phase
Add Drug, which is
dissolved in suitable
solvent
10
Parameter Importance Method
Size and Shape Determine skin penetration SEM, TEM, Dynamic
Light Scattering
Zeta potential Stability of vesicles Zeta Sizer
Entrapment
efficiency
Suitability of method Ultracentrifugation
and HPLC
Drug content Important in deciding the amount of vesicle
preparation to be used
UV, HPLC
Stability studies To determine the shelf life of vesicle formulation SEM, TEM, HPLC
In vitro dissolution Determine the drug release rate from vesicle Franz diffusion cell
Skin permeation Determines rate of drug transport through skin Confocal Laser
Scanning Microscopy
11
Enhanced permeation of drug through skin for transdermal drug delivery
Delivery of large molecules (peptides, protein molecules) is possible
It contains non‐toxic raw material in formulation
Ethosomal drug delivery system can be applied widely in Pharmaceutical,
Veterinary, Cosmetic fields
Simple method for drug delivery in comparison to Iontophoresis and
Phonophoresis and other complicated methods
High patient compliance‐ The ethosomal drug is administrated in semisolid
form (gel or cream) hence producing high patient compliance
12
DRUG APPLICATION ADVANTAGE
Minodixil Hair growth promotion Higher skin retention
Cannabidol Prevents inflammation and
edema
Significant accumulation
of the drug in the skin
Bacitracin Treatment of dermal
infections
Reduced drug toxicity
Acyclovir Treatment of Herpetic
infection
Improved drug delivery
13
Ethosomal administration is not a means to achieve rapid bolus type drug
input, rather it usually designed to offer slow, sustained drug delivery
The molecular size of the drug should be reasonable that it should be
absorbed percutaneously
Adhesive may not adhere well to all types of skin
May not be economical
Poor yield
Skin irritation or dermatitis due to excipients and enhancers of drug
delivery systems
14
15
The main limiting factor of transdermal drug delivery system is epidermal
barrier can be overcome by ultra deformable vesicles to significant extent
They are emerging vesicular carrier because they have site specificity, high
penetration power, higher deformability and higher stability
16
19

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Ethosome

  • 1. ETHOSOMES Presented By: Saurabh sharma 2nd Semester Pharmaceutics School Of Pharmaceutical Sciences Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Road, Gandhi Nagar, Bhopal Session 2018- 2020 1
  • 2. Flow of Presentation • Introduction • Types of ethosomes • Mechanism of ethosome • Additives used in ethosome • Method of preparation • Characterization of ethosome • Advantages and limitations • Summary
  • 3. Ethosomes are ethanolic liposomes The ethosomes are vesicular carriers consisting of hydroalcoholic or hydroglycolic phospholipids in which the concentration of alcohols or their combination is relatively high. These are soft, malleable vesicles tailored for enhanced delivery of active agents. Ethosomes which are novel permeation-enhancing lipid vesicles embodying high concentration (20–45%) of ethanol 1
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  • 7. Ethanol effect  Ethanol acts as a penetration enhancer through the skin. Ethanol penetrates into intercellular lipids and increases the fluidity of cell membrane lipids and decrease the density of lipid multilayer of cell membrane Ethosomes effect  Ethosomes permeates very easily inside the deep skin layers, where it got fused with skin lipids and releases the drugs into deep layer of skin 5
  • 9. CLASS EXAMPLES USES Phospholipid Soya phosphatidylcholine, Egg phosphatidylcholine, Dipalmityl phosphatidylcholine, Distearyl phosphatidylcholine Vesicles forming component Polyglycol Propylene glycol, Transcutol As a skin penetration enhancer Alcohol Ethanol, Isopropyl alcohol For providing the softness for vesicle membrane, as a penetration enhancer Cholesterol Cholesterol For providing the stability to vesicle membrane Dye Rhodamine-123, Rhodamine Red, Fluorescene Isothiocynate (FITC), 6- Carboxy fluorescence For characterization study Vehicle Carbopol Ð934 As a gel former 7
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  • 12. Disperse phospholipid in water at 40˚C Ethanol + propylene glycol at 40˚C Mix organic phase to aqueous phase Add Drug, which is dissolved in suitable solvent 10
  • 13. Parameter Importance Method Size and Shape Determine skin penetration SEM, TEM, Dynamic Light Scattering Zeta potential Stability of vesicles Zeta Sizer Entrapment efficiency Suitability of method Ultracentrifugation and HPLC Drug content Important in deciding the amount of vesicle preparation to be used UV, HPLC Stability studies To determine the shelf life of vesicle formulation SEM, TEM, HPLC In vitro dissolution Determine the drug release rate from vesicle Franz diffusion cell Skin permeation Determines rate of drug transport through skin Confocal Laser Scanning Microscopy 11
  • 14. Enhanced permeation of drug through skin for transdermal drug delivery Delivery of large molecules (peptides, protein molecules) is possible It contains non‐toxic raw material in formulation Ethosomal drug delivery system can be applied widely in Pharmaceutical, Veterinary, Cosmetic fields Simple method for drug delivery in comparison to Iontophoresis and Phonophoresis and other complicated methods High patient compliance‐ The ethosomal drug is administrated in semisolid form (gel or cream) hence producing high patient compliance 12
  • 15. DRUG APPLICATION ADVANTAGE Minodixil Hair growth promotion Higher skin retention Cannabidol Prevents inflammation and edema Significant accumulation of the drug in the skin Bacitracin Treatment of dermal infections Reduced drug toxicity Acyclovir Treatment of Herpetic infection Improved drug delivery 13
  • 16. Ethosomal administration is not a means to achieve rapid bolus type drug input, rather it usually designed to offer slow, sustained drug delivery The molecular size of the drug should be reasonable that it should be absorbed percutaneously Adhesive may not adhere well to all types of skin May not be economical Poor yield Skin irritation or dermatitis due to excipients and enhancers of drug delivery systems 14
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  • 18. The main limiting factor of transdermal drug delivery system is epidermal barrier can be overcome by ultra deformable vesicles to significant extent They are emerging vesicular carrier because they have site specificity, high penetration power, higher deformability and higher stability 16
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