TRANSFERSOMES

Meetali MudgilM-Pharmacy 2nd Sem.ID NO. M100400007.

CONTENTS

• Introduction• Salient features• Limitations• Material used • Method of preparation and• Mechanism of penetration.

Introduction Transfersome is a term registered as a trademark by

the German company IDEA AG. The targeted analgesic Diractin® (ketoprofen in Transfersom®

gel) is Company’s lead product, addressing the large market for peripheral pain.

The concept was introduced in 1992 by Cevc and co-workers. They were introduced for the effective transdermal delivery of

number of low and high molecular weight drugs. Transfersomes are a special type of liposomes, consisting of

phosphatidylcholine and an edge activator. Introduced to overcome the permeability problems of

liposomes & niosomes.

These vesicular transfersomes are several orders of magnitude more elastic than the standard liposomes and thus well suited for the skin penetration .

A Transfersomes, in functional terms, may be described as lipid droplets of such deformability that permits its easy penetration through the pores much smaller than the droplets size.

They overcome the skin penetration difficulty by squeezing themselves along the intracellular sealing lipids of the stratum corneum.

Flexibility of transferosomes membrane is achieved by mixing suitable surface active components in the proper ratios.

They penetrate the stratum corneum either by intracellular route or by transcellular route.

Salient features of transferosomes:

1. The Transferosomes are biocompatible & biodegradable.

2. In case of lipophilic drugs the entrapment efficiency is very high near to 90%.

3. It is now widely used as a novel carrier for both systemic as well as topical delivery of drugs.

4. They protect the encapsulated drug from metabolic degradation.

5. They can act as a carrier for low as well as high molecular weight drugs e.g analgesics, anesthetics, corticosteroids, insulin, albumin , anticancer agents.

6. The resulting flexibility of transfersomes membrane minimize the risk of complete vesicle rupture in the skin and allow transfersomes to follow the natural water gradient across the epidermis ,when applied under non occlusive condition.

7. They act as depot, releasing their content slowly and gradually.

8. They possess an infrastructure consisting of hydrophobic and hydrophillic moieties together and as a result can accommodate drug molecules with wide range of solubility.

Limitations

They are chemically unstable because of their predisposition to oxidative degradation.

Purity of natural phospholipids is another criteria against adoption of transfersomes as drug delivery vehicles.

Transfersomes formulations are expensive.

Materials usedCLASS EXAMPLE USES

Phospholipid Soya phosphatidyl choline,egg phosphatidyl choline,dipalmitoyl phosphatidyl choline

Vesicles forming component.

Surfactant Sod.cholate,Sod.deoxycholate,Tween-80,Span-80

For providing flexibility

Alcohol Ethanol, methanol As a solvent

Buffering Agent Saline phosphate buffer (pH 6.4)

As a hydrating medium

Phospholipids

Method of preparation

Surfactant

Dissolve in organic solvent Incorporate liphophillic drug

Prepare thin film(using rotary evaporator)

Keep under vacuum(12hr)

Hydrate using buffer(pH6.5) at 60 rpm

Homogenize (extrusion 10 times through a sandwitch of 200 & 100 nm polycarbonate memb)

Sonicate (30 min)Using bath or probe sonicator at 380W

Incorporate Hydrophillic drug

TRANSFEROSOMES

Mechanism of penetration of Transfersomes

Transfersomes when placed on skin surface

Dehydrated by water evaporation loss

Lipid vesicles feels “osmotic gradient”

Move along this gradient, deform to pass through narrow pores in skin

References

o Pirvu C.D., Hlevca C., Ortan A., Prisada R.; Farmacia; Vol 58; Issue 2; 2010; Elastic Vesicles as Drugs Carriers Through The Skin; Pg 128-135

o Patel R., Singh S.K., Singh S., Sheth N.R., Gendle R.; Journal of Pharmaceutical Sciences & Research; Vol 1; Issue 4; 2009; Development & Characterization of Curcumin Loaded Transferosome for Transdermal Delivery; Pg: 71-80

o Jain N.K., Advances in Controlled & Novel Drug Delivery, CBS publishers; 1st edition ; p: 426 – 451

o Saraf S.; Pharmainfo.net: Vol 5; Issue 6; Transferosomes : An Overview; 12/30/2007