Ethosomes and Transethosomes

1. ETHOSOME AS NOVEL DRUG DELIVERY SYSTEM
DEPARTMENT OF PHARMACEUTICS
Presented BY- Ankit Sharma
ROLL NO-05
P.D.E.A’s S.G.R.S college of Pharmacy Saswad

2. CONTENTS
•Introduction
•Definition
•Composition
•Marketed Preparation
•Mechanism of action
•Advantages & Disadvantages
•Characterization
•Method of preparation
•Evaluation
•Application
•Reference 2

3. DEFINITION
Ethosomes are non-invasive delivery carriers
that enable drugs to reach the deep skin
layers and/or the systemic circulation.
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4. STRUCTURE OF ETHOSOMES
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5. COMPOSITION
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Class Example Uses
1.
Phospholipids Soya Lecithin Vesicles forming component
2.
Polyglycol Propylene
glycol
As a skin penetration
enhancer
3.
Alcohol Ethanol For providing the softness
for vesicle membrane
4.
Cholesterol Cholesterol
For providing the stability to
vesicle membrane

6. Marketed Preparation
6
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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 pee
Nottingham, UK
4. Supravir cream For the treatment of herpes virus Trima,Israel

7. MECHANISM OF ACTION
The drug absorption probably occurs in following two phases:
1. Ethanol effect
2. Ethosomes effect
1. Ethanol effect
Ethanol acts as a penetration enhancer through the skin. The
mechanism of its penetration enhancing effect is well known.
Ethanol penetrates into intercellular lipids and increases the
fluidity of cell membrane lipids and decrease the density of
lipid multilayer of cell membrane.
2. Ethosomes effect
Increased cell membrane lipid fluidity caused by the ethanol
of ethosomes results 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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9. ADVANTAGES
1. Delivery of large molecules (peptides) is possible.
2. It contains non-toxic raw material in formulation.
3. Ethosomal drug delivery system can be applied widely in
pharmaceutical veterinary, cosmetic fields.
4. Ethosomes enhance permeation of the drug through
skin transdermal & dermal delivery.
5. Low risk profile.
6. High patient compliance.
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10. DISADVANTAGES
1. Poor Yield.
2. Loss of product during transfer from organic to water
media.
3. Drug that require high blood levels can not be
administrated- limited only to potent molecules, those
requiring a daily dose of 10mg or less.
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11. CHARACTERIZATION
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s
Importance Method
1. Size and shape Determine skin
penetration
SEM, TEM, DLS
2. Zeta potential Stability of vesicles Zeta Meter
3. Entrapment
efficiency
Suitability of method Ultracentrifugation
4. Drug content Important in deciding
the amount of vesicle
preparation to be used
UV, HPLC
5. Stability studies To determine the shelf
life of vesicle formulation
SEM, TEM, HPLC
6. In vitro
dissolution
Determine the drug
release rate from vesicle
Franz diffusion cell
7. Skin permeation Determines rate of drug
transport through skin
CLSM

12. Method of Preparation
1. Cold method
2. Hot method
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13. COLD METHOD
In this method Phospholipids, drug and other lipid materials
are dissolved in ethanol in a covered vessel at room
temperature by vigorous stirring with the use of mixer.
Propylene glycol or other polyol is added during stirring. This
mixture is heated to 3000
C
a water bath. The water heated to
3000C
in a separate vessel is added to the mixture, which is
then stirred for 5 min in a covered vessel. The vesicle size of
ethosomal formulation can be decreased to the desire extent
using probe sonication or extrusion method. Finally, the
formulation is stored under refrigeration.
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14. 14

15. HOT METHOD
In this method Phospholipid is dispersed in water by heating
in a water bath at 4000
C until a colloidal solution is obtained.
In a separate vessel ethanol and propylene glycol are mixed
and heated to 4000 C
. Once both mixtures reach 400
C the
organic phase is added to the aqueous one. The drug is
dissolved in water or ethanol depending on its hydrophilic or
hydrophobic properties. The vesicle size of ethosomal
formulation can be decreased to the desire extent using probe
sonication or extrusion method.
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16. Evaluation
1. Filter Membrane- Scanning Electron Microscopy Vesicle
suspension (0.2 mL) was applied to filter membrane having a
pore size of 50 nm and placed in diffusion cells.
*The upper side of the filter was exposed to the air, whereas the
lower side was in contact with PBS (phosphate buffer saline
solution), (pH 6.5).
*The filters were removed after 1 hour and prepared for SEM
studies by fixation at 4°C in Karnovsky’s fixative overnight
followed by dehydration with graded ethanol solutions (30%,
50%, 70%, 90%, 95%, and 100% vol/vol in water).
*Finally, filters were coated with gold and examined in SEM.
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17. 2. Vesicle-Skin Interaction Study by TEM and SEM From
animals ultra thin sections were cut (Ultra cut, Austria),
collected on fervor-coated grids and examined under
transmission electron microscope. For SEM analysis, the
sections of skin after dehydration were mounted on stubs
using an adhesive tape and were coated with gold palladium
alloy using a fine coat ion sputter coater. The sections were
examined under scanning electron microscope.
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18. Application
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Drug Purpose of Ethosomal
delivery
Application
1. Diclofenac Selective targeting the cells NSAIDS
2. Zidovudine Better cellular uptake Anti‐HIV
3. Trihexyphenidyl
hydrochloride
4.5‐times higher than that from
liposome
Treatment of
Parkinson’s disease
4. Ammonium
glycyrrhizinate
Poor skin permeation Poor oral
bioavailability
Treatment of
inflammatory
based skin
diseases
5. Salbutamol Enhanced drug delivery through
skin with ethosomes
Anti‐asthmatic
6. Cannabidol
(CBD)
Improved skin deposition
Improved biological activity
Antibiotic
7. Cyclosporine Poor oral absorption and
bioavailability.
Treatment of
Inflammatory skin
disease
8. Bacitracin Reduced drug toxicity. Treatment of
dermal infections

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9. Insulin Improved therapeutic efficacy
of drug
Treatment of Diabetes
Improved therapeutic
efficacy of drug.
10. Minoxidil High penetration into the
deep skin layer
Piloscabeous targeting

20. Transethosomes
Several strategies have been used in order to overpass the stratum
conium (SC) barrier. Among other drug delivery systems, liposome's
were used for topical drug delivery.
1 Liposome's are typically hollow spheres surrounded by a lipid
doubled layer. Once applied on skin surface, they only remain in the
upper layer of the SC, acting as a drug reservoir.
2 Thus, due to their unstable nature and poor skin permeability,
they are only suitable for topical drug delivery.
3 As UDV are more deformable than conventional liposome's, they
have demonstrated a great ability to cross the intact skin and
deliver the loaded drugs into the epidermis and dermis layers or
even to the systemic circulation. Phospholipids, ethanol, bile salts,
and many surfactants have been used for the preparation of these
elastic
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21. Advantages
1. Nontoxic
2. Thermodynamically stable formulations.
3. They have been used for dermal and
transdermal delivery of many molecules
including peptides and proteins.
4. In addition, their production is relatively
simple and easy to scale up.
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22. Comparison
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Characteristics Transethosomes Ethosomes
1. Vesicles 2nd generation elastic lipid
vesicles carrier
3rd generation elastic
lipid vesicle carrier
2. Composition Phospholipids & edge
activator
Phospholipids &
ethanol
3. Characteristics Ultra flexible liposome's Elastic liposome's
4. Flexibility High deformability due to
surfactant
High deformability &
elasticity due to ethanol
5. Permeation
Mechanism
Deformation of vesicle Lipid perturbation

23. Reference
1.Sivakranth M., AnjumaAra P., Krishnaveni C.,
Venkatesh E., Ethosomes: A Novel Vesicular
Drug Delivery System, International Journal of
Advances in Pharmaceutical Research
2012;2,1:16-27.
2. Sachan R., Bajpai M., Transdermal Drug
Delivery System: A Review, International Journal
of Research and Development in Pharmacy and
Life Sciences 2013;31:748-765
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24. 3. Dhurve R., Kashyap N., Mishra A., Kumar Pathak
A., A Holistic Review on Ethosome: A Promising Drug
Delivery System for Topical Fungal Disease,
International Journal of Pharmaceutical & Biological
Archives 2014;5,5:13-26.
4. Celia C., Cilurzo F., Trapasso E., Cosco D., Fresta M.,
Paolino D., Ethosomes and Transfersomes Containing
Linoleic Acid: Physicochemical And Technological
Features of Topical Drug Delivery Carriers For The
Potential Treatment of Melasma Disorders,
Biomedical Microdevices 2011;6:105-111.
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25. 5. Rakesh R., Anoop KR., Ethosome for
Transdermal and Topical Drug Delivery,
International Journal of Pharmaceutical
Sciences and Research 2012;4,3:17-24.
6. Jain H., Patel J., Joshi K., Patel P., Upadhyay
UM., Ethosomes: A Novel Drug Carrier,
International Journal of Clinical Practice
2011;7:1:1-4.
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