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TRANSFERSOMES

Meetali 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 EXAMPLE USES
Phospholipid Soya phosphatidyl Vesicles forming  
choline,egg     component.
phosphatidyl
choline,dipalmitoyl
phosphatidyl choline

Surfactant Sod.cholate,Sod.deoxyc For providing flexibility


holate,Tween-80,Span-
80

Alcohol Ethanol, methanol As a solvent

Buffering Agent Saline phosphate As a hydrating medium


buffer   (pH 6.4)
Method of preparation

Phospholipids Surfactant

Dissolve in organic solvent Incorporate liphophillic


drug

Prepare thin film


(using rotary evaporator)
Keep under vacuum
(12hr)

Hydrate using buffer Incorporate


(pH6.5) at 60 rpm 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

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