This document discusses transfersomes, a novel lipid-based vesicular system for transdermal drug delivery. Transfersomes can penetrate the skin through intracellular or transcellular routes due to their elastic and deformable nature. They have advantages like accommodating both hydrophilic and hydrophobic drugs, achieving high skin penetration ability due to flexibility. The document covers transfersome formulation methods, characterization techniques, mechanisms of penetration, marketed products, and concludes they are a promising system for transdermal delivery of a wide range of drugs.
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Transfersomes
1.
2. 1.) Introduction
2.) Novel Method in Transdermal Drug Delivery system
3.) Transfersomes
4.) Advantage
5.) Disadvantage
6.) Mechanism of Penetration
7.) Formulation Consideration
8.) Preparation of Transfersomes
9.) Characterization of Transfersomes
10.) Application
11.) Marketed Formulation worldwide
12.) Conclusion
3. Lipid based vesicular system are able to pass through
narrow pathways between skin cells to mediate drug
transport containing hydrophilic and hydrophobic drugs
in the aqueous core as well as vesicle bilayer.
Transfersome are a form of elastic or deformable
vesicle ,which were introduced in the early 1990’s
These elastic vesicles are also known as
flexible vesicles etc.
4. Transfersome penetrate the stratum corneum by either
intracellular route or the transcellular route.
Transfersomes dose is applied perunit skin surface
area,rather than the total drug amount or concentration.
Transfersomes components that sustain strong membrane
deformation preferentially accumulate while the less
adaptable molecule are diluted at sites of great stress.
Flexibility of transfersomes memebrane is achieved by
mixing suitable surface –active components.
5. Accommodate drug molecule with wide range of
solubility.
High deformability permits better penetration on intact
vesicles.
They can carry low as well as high molecular weight
drugs.
They are biocompatible and biodegradable.
They have high entrapment efficiency
6. Transfersomes are chemically unstable.
Commercialization on large scale is difficult due to
oxidative degradation.
Lack of Purity of natural phospholipids.
Transfersome formulation are expensive.
7. Transfersomes can penetrate the skin by the mechanism
known as osmotic gradient generation due to evaporation of
water when applied in the form of lipid suspension on the
skin surface.
8. Materials used in formulation of transfersomes are-
1.) Phospholipid – Used as an vesicle forming component.
Eg- Soya Phosphatidylcholine
2.) Surfactant- Used as flexibility provider
Eg- Sodium cholate
3.) Alcohol – Used as Solvent.
Eg- Ethanol
4.) Dye – Used for confecal scanning laser microscopy.
Eg- Rhodamine-123
9. 5.) Buffering Agent – Used as hydrating medium
Eg- Saline phosphate buffer (PH6.1)
Basically 2 methods are used-
1.) Vortexing- sonication Method
2.) Rotary evaporation sonication Method
10.
11.
12. Vesicle Shape ,Diameter and Type
In- vitro drug release
Entrapment efficiency
Number of vesicles per cubic mm
surface charge, Charge density,
Degree of deformability or permeability measurement
13. Improved transdermal flux – Cancer treatment (Vincristine)
Improved site specificity – Skin diseases
(corticosteriods)
Non- Invasive immunization –Immunization( (Soluble
protein)
Improved drug stability –Hydrocortosone
Non-invasive treatment of local pain through topical route-
Tetracaine
15. S.No Name of Product Drug Use
1. Daktarin Miconazole nitrate Antifungal
2. Flexiseq Ketoprofen Oeteoarthritis
3. Voltaren Diclofenac sodium NAID’s
4. Sporanox Itraconazole Antifungal
5. Timoptol-XE Timolol Maleate Non selective beta
adrenergic receptor
antagoinst
6. Diracetin Ketoprofen Oeteoarthritis
16. These ultra-deformable system hold great potential in
delivery of enormous range of drug substances, which
include large molecule like peptides,hormones and
antibotics
It is evident that transfersomes hold promise for
overcoming the barrier properties of the stratum
corneum