2. Contents
• Introduction
• Advantages
• Disadvantages
• Mechanism of penetration of ethosomes
• Composition of ethosomes
• Formulation of ethosomes
• Particle size determination
• Marketed formulations
• Future aspects
• References
3. Introduction
• Ethosomes are soft lipid vesicles made up of phospholipids,
ethanol and water.
• It can entrap drug molecules of various physical and
chemical characteristics i.e., hydrophilic, lipophilic or
amphiphilic.
• The size range of ethosomes may vary from 10 nanometers
to microns.
• In 1996, Touitou discovered and investigated lipid
vesicular system containing ethanol in concentration range
10-50%.
• These are non invasive delivery carriers that enable drugs
to reach the deep skin layers and/or systemic circulation.
4. Advantages
• Delivery of large molecules is possible (peptides, protein molecules)
• Enhanced permeation of drug through skin for transdermal drug delivery.
• High patient compliance.
• Simple method for drug delivery.
• It is passive, non invasive and is available for immediate commercialization.
Disadvantages
• May not be economical, poor yield.
• Drugs that require high blood levels cannot be administered – limited to only potent drugs,
those requiring a daily dose of 10 mg or less.
• Coalescence of ethosomes may occur.
5. Mechanism of penetration of ethosomes
The advantages of ethosomes over liposomes are increased permeation of the drugs. The drug
absorption occurs in following two phases.
Ethanol effect
• Ethanol acts as penetration enhancer
through skin.
• Ethanol penetrates into intercellular
lipids and increases the fluidity of cell
membrane lipids and decrease the
density of lipid multilayer of cell
membrane.
Ethosome effect
• Increased cell membrane lipid fluidity
due to ethanol.
• Increased skin permeability.
• So the ethosomes permeated very easily
inside the deep skin layers, where it gets
fused with skin lipids and releases the
drugs.
6.
7. Composition of ethosomes
Class Use
Phospholipid Vesicle forming component
Alcohol For providing softness for vesicle
membrane also as a penetration enhancer
Polyglycol As a skin penetration enhancer
cholesterol Enhances the stability and entrapment
efficiency of drugs
8. Formulation of ethosomes
• Ethosomes were prepared as reported by Touitou et al.; lecithin (3% w/v) was taken in a
small round bottom flask and solubilized with ethanol (50% v/v) under mixing with a
magnetic stirrer at 30°C.
• The round bottom flask was covered to avoid ethanol evaporation.
• Distilled water was added slowly with continuous stirring at 700 rpm to obtain the
ethosomal colloidal suspensions.
• Finally it was sonicated for 15 minutes.
9. Ethanol + Phospholipid
(at 30°C)
Distilled water
(at 30°C)
At 700 rpm Ethosomes of irregular
size range were obtained
Ethosomes of regular
size range were obtained
Sonicated
for 15
minutes
10. Particle size determination
• Nicomp® Nano DLS/ZLS System was used for
particle size determination.
• Small amount of sample was run for particle size
determination and the particle size of ethosome
came out to be 762 nm.
11.
12. Marketed formulations
Sr.
no.
Name of
product
Uses Manufacturer
1. Decorin cream Anti-aging cream, treating,
repairing, and delaying the visible
aging signs of the skin including
wrinkle lines
Genome
Cosmetics
2. Nanominox First minoxidil containing product,
which uses ethosomes. Contains
4% Minoxidil, well- known hair
growth promoter that must be
metabolized by sulfation to the
active compound
Germany
3. Skin genuity Powerful cellulite buster, reduces
orange peel
Nottingham, UK
4. Supravir cream For the treatment of herpes virus Trima,Israel
13. Future aspects
• Introduction of ethosomes has initiated a new area in vesicular research for transdermal
drug delivery.
• Different reports show a promising future of ethosomes in making transdermal delivery
of various agents more effective.
• Further, research in this area will allow better control over drug release in vivo, allowing
physician to make the therapy more effective.
• Ethosomes offers a good opportunity for the non-invasive delivery of small, medium and
large sized drug molecules.
• The results of the first clinical study of acyclovir-ethosomal formulation support this
conclusion.
• Thus, it can be a logical conclusion that ethosomal formulations possess promising future
in effective 33 dermal/transdermal delivery of bioactive agent.
14. References
• CH Kumar Ananda, Dutt Rajeswar, Ethosomes: A Novel Transdermal Drug Delivery System, American
Journal of Pharmaceutical Sciences, 2014.
• E. Touitou, N. Dayan, L. Bergelson, B. Godin, M. Eliaz, Ethosomes — novel vesicular carriers for
enhanced delivery: characterization and skin penetration properties, Journal of Controlled Release
65 (2000) 403–418.
• Ibrahim M Abdulbaqi, Yusrida Darwis, Nurzalina Abdul Karim Khan, Reem Abou Assi, Arshad A Khan,
Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties,
in vivo studies, and clinical trials, Int J Nanomedicine. 2016; 11: 2279–2304.
