TRANSFEROSOMES meet

TRANSFERSOMESMeetali Mudgil M-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 used CLASS Phospholipid EXAMPLE Soya phosphatidyl choline,egg phosphatidyl choline,dipalmitoyl phosphatidyl choline Sod.cholate,Sod.deoxyc holate,Tween-80,Span80 Ethanol, methanol Saline phosphate buffer (pH 6.4) USES Vesicles forming component.

Surfactant

For providing flexibility

Alcohol Buffering Agent

As a solvent As a hydrating medium

Method of preparation Phospholipids Surfactant

issolv in organic solv nt

Incorporat liphophillic drug

Pr par thin film (using rotary vaporator)

Keep under vacuum (12hr)

Hydrate using buffer (pH6.5) at 60 rpm

Incorporate Hydrophillic drug

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

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

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