2. Ethosomes
A NOVAL DRUG DELIVERY SYSTEM
Presented by
Shrikant Potdar
M. Pharm
Pharmaceutics sem
III rd
Guided by
Dr. Madhur Kulkarni
Associate professor
Indira college of Pharmacy, Pune. 2
3. Contents
■ Introduction : Ethosomes
■ Advantages & Disadvantages
■ Mechanism of penetration
■ Composition of ethosomes
■ Methods of preparation
■ Characterization of ethosomes
■ Application
■ Future Aspects
■ Conclusion
■ References
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4. Ethosomes
■ Ethosomes are non-invasive delivery carriers that enable drugs to reach the deep
skin layers and/or the systemic circulation.
■ soft vesicles made of phospholipids and ethanol (in higher quantity) and water.
■ The size range of ethosomes may vary from tens of nanometers to microns (µ).
■ In 1996 Touitou discovered and investigated lipid vesicular system containing
ethanol inrelatively high concentration (20-50%).
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7. Advantages
Enhanced permeation of drug through skin for transdermal drug delivery.
Delivery of large molecules (peptides, protein molecules] is possible.
High patient compliance- Can used in the form of gel, cream and patch.
Simple method for drug delivery in comparison to Iontophoresis and
Phonophoresis and other complicated methods.
Better stability and solubility of many drug as compared to other conventional
vesicles.
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8. Disadvantages
• If shell locking is ineffective then the coalescence of ethosomes may occurs
and fall apart on transfer into water.
• Loss of product during transfer from organic phase to water media
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9. Mechanism of penetration
The main advantage of ethosomes over liposomes is the increased permeation
of the drug.
Two
phases
Ethosomes
effect
Ethanol
effect
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10. 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.
Ethosome
effect
• Increased cell membrane lipid fluidity due to
ethanol.
• increased skin permeability
• So the 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
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11. (A) Normal skin;
(B) Skin-lipid perturbation by ethanol effects;
(C) Penetration of the soft malleable ethosomal system vesicles.
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12. Composition of ethosomes
Class Use
Phospholipid Vesicles forming component
Alcohol (Ethanol Isopropyl alcohol )
For providing the softness for vesicle
membrane
As a penetration enhancer
Polyglycol (Propylene glycol)
As a skin penetration enhance
Edge activators or penetration enhancers
Cholesterol
Enhances the stability and entrapment
efficiency of drugs
Vehicle
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17. phospholipid is dispersed in water by heating in a water bath at 40˚c until a colloidal solution is
obtained
In another vessel, ethanol is heated to 40°c
added dropwise to the phospholipid dispersion under continuous mixing using a mechanical or magnetic
stirrer
The drug is dissolved in either the organic or aqueous phase, based on its hydrophilic/hydrophobic
properties.
Hot Method
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18. Characterization
1) Visualization
2) Vesicle size and Zeta potential
3) Transition Temperature
4) Surface Tension Activity Measurement
5) Entrapment Efficiency
6) Penetration and Permeation Studies
7) Vesicle Stability
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19. Characterization
1) Visualization: Visualization of ethosomes can be done using transmission
electron microscopy (TEM) and by scanning electron microscopy (SEM
TEM (magnification 315 000) SEM (magnification 100 000)
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20. 2) Vesicle size and Zeta potential:
• Particle size and zeta potential can be determined by dynamic light scattering
(DLS) using a computerized inspection system and photon correlation
spectroscopy (PCS).
• As the alcohol concentration increases the vesicular size decreases.
• As the phospholipid concentration increases the vesicular size also increases
Characterization
3) Transition Temperature:
• The transition temperature of the vesicular lipid systems can be determined by
using differential scanning calorimetry (DSC).
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22. Entrapment Efficiency :
• The entrapment efficiency of drug by ethosomes can be measured by the ultra
centrifugation technique
Penetration and Permeation Studies:
• Depth of penetration from ethosomes can be visualized by confocal laser scanning
Vesicle Stability:
• The stability of vesicles can be determined by assessing the size and structure of the
vesicles over time. Mean size is measured by DLS and structure changes are observed
by TEM
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26. Future Aspects
• Introduction of ethosomes has initiated a new area in vesicular research
for transdermal drug delivery.
• Different reports shows a promising future of ethosomes in making TDD of
various agent more effective.
• Further research in this area allow better control over drug release in vivo,
allowing physician therapy more effective.
• Ethosomes offers a good opportunity for non-invasive delivery of drug
delivery of small, medium, large drug molecules.
• The results of the first clinical study of acyclovir ethosomal formulation
supports this conclusion.
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27. Conclusion
• It has been almost 2 decades since the invention of ethosomes, and during this period
these nanocarriers have proven their unique ability to deliver therapeutic agents of
different physicochemical properties through the skin for local and systemic use.
• The incorporation of ethosomal systems in suitable vehicles such as gels, patches, and
creams represents an important step to get better skin-permeation and therapeutic
results. 27
28. Referances
1. Touitou E, Dayan N, Bergelson L, Godin B, Eliaz M. Ethosomes — novel vesicular carriers for enhanced
delivery: characterization and skin penetration properties. J Control Release. 2000;65(3):403–418.
2. Fang YP, Tsai YH, Wu PC, Huang YB. Comparison of 5-aminolevulinic acid-encapsulated liposome
versus ethosome for skin delivery for photodynamic therapy. Int J Pharm. 2008;356(1–2):144–152.
3. Verma P, Ram A. Effect of different penetration enhancers on skin permeation of drug using
ethosomal carrier systems. J Curr Pharm Res. 2011;5(1):42–44.
4. Shen S, Liu SZ, Zhang YS, et al. Compound antimalarial ethosomal cataplasm: preparation, evaluation,
and mechanism of penetration enhancement. Int J Nanomedicine. 2015;10:4239–4253.
5. Marco B, Natascia M, Francesca E, Marzia C, Paola M. Comparative study of liposomes, transfersomes
and ethosomes as carriers for improving topical delivery of celecoxib. Drug Delivery 2012; 19(7): 354–
361.
6. Tarun P, Soniya, Sachan R, SinghV, Singh G, Tyagi S, Patel C, Gupta A. Ethosomes: a recent vesicle of
transdermal drug delivery system. I J Res and Dev in Pharm Life Sci. 2013; 2(2): 285-292
7. Zhu X, Li F, Peng X, Zeng K. Formulation and evaluation of lidocaine base ethosomes for transdermal
delivery. Anesth Analg. 2013;117(2):352–357.
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most common and widely used method
Dissolve phospholipid, drug and other lipid materials in ethanol in a covered vessel at room temperature with vigorous stirring. Add propylene glycol or other polyol during stirring.