Transferosomes are a novel vesicular drug carrier system composed of phospholipids, surfactants, and water that can enhance transdermal drug delivery. They are highly flexible and deformable, allowing them to squeeze through the skin's layers more easily than other carriers. Transferosomes can transport both low and high molecular weight drugs into or through the skin, depending on the application method. They are prepared using phospholipids that form lipid bilayers, along with edge activators that increase bilayer flexibility. Transferosomes have advantages like high drug entrapment efficiency, protection of drugs from degradation, and ability to deliver a wide range of drug molecules. They have potential applications in controlled drug release and delivery of proteins, peptides, and other large

1. TRANSFEROSOMES
Presented by-
Sushmita Gupta
M.Pharmacy
Industrial Pharmacy
Acharya & B.M.Reddy College of Pharmacy

2. Contents
 Introduction
 Structure and composition
 Advantages and limitations
 Mechanism of drug penetration
 Method of preparation
 Characterisation
 Applications
 References

3. Introduction
 Transferosome is a novel , elastic or ultradeformable
vesicular drug carrier system composed of phospholipid,
surfactant and water for enhanced transdermal delivery.
 It overcomes the filtration and skin penetration difficulty
by squeezing themselves along the intracellular sealing
lipid of the stratum corneum.
 Because of their self optimised and ultraflexible
membrane properties, they are able to deliver a low and
high molecular weight drug either into or through the
skin depending upon the choice of administration or
application.
 The resulting flexibility of transferosomes membrane
minimises the risk of complete vesicular rupture in the
skin and allow them to follow the natural water gradient
across the epidermis.

4. Structure and composition
 Transfersomes is composed of phospholipids like
phosphatidylcholine which self assembles into lipid
bilayer in aqueous environment and closes to form a
vesicle.
 A lipid bilayer softening component ( biocompatible
surfactant or an amphiphilic drug) is added to increase
lipid bilayer flexibility and permeability and known as edge
activator.
 An edge activator consists usually of single chain
surfactant of non ionic nature that causes destabilization
of the lipid
bilayer thereby increasing its fluidity and elasticity .
 Flexibility of transfersomes membrane can be altered by
mixing suitable surface active agents in the proper ratios.

7. Advantages
 Transfersomes possess an infrastructure consisting of
hydrophobic and hydrophilic moieties together and as a
result can accommodate drug molecules with wide
range of solubilities.
 They are biocompatible and biodegradable as they are
made from natural phospholipids similar to liposomes.
 They have high entrapment efficiency, in case of
lipophilic drug near to 90%.
 This high deformability gives better penetration of intact
vesicles.
 They can act as a carrier for low as well as high
molecular weight drugs eg. analgesic,
anesthetic,corticosteroids, sex hormone, anticancer,
insulin, gap junction protein, and albumin.

8.  They act as depot, releasing their contents slowly and
gradually.
 They can be used for both systemic as well as topical
delivery of drug.
 They protect the encapsulated drug from metabolic
degradation.
 Scale up procedure is simple and easy, hence avoids
unnecessary use of pharmaceutically unaccepted
additives.

9. Limitations
 Transfersomes are chemically unstable because of their
predisposition to oxidative degradation.
 Purity of natural phospholipids is another criteria
militating against adoption of transfersomes as drug
delivery vehicles.
 Transfersomes formulations and manufacturing aspects
are expensive.

10. Mechanism of drug penetration
The mechanism of drug penetration can be described in
three purposed mechanisms.
 Interaction between the lipid residue and the proximal
water makes the lipid to attract water molecules
inducing hydration and the lipid vesicles move to the site
of higher water concentration. This difference in water
content across the skin strateum and epidermis
develops transdermal osmotic gradient leading to
penetration of transferosomes across the skin.

11.  Tranferosomes act as permeation enhancers that disrupt
the intercellular lipid from the stratum that ultimately
widens the pores and facilitates the molecular interaction
and penetration of system across the skin.
 Tranferosomes by enforcing its own route induce
hydration that widens the hydrophilic pores of the skin
causing the gradual release of the drug that bind to the
target organ.

13. Method of preparation
 A thin film is prepared ,hydrated and then brought to the
desired size by sonication. Sonicated vesicles are
homogenized by extrusion through a polycarbonate
membrane.
 The mixture of vesicles forming ingredients(
phospholipids and surfactant) were dissolved in volatile
organic solvent (chloroform-methanol).
 Organic solvent was evaporated above the lipid
transition temperature using rotary evaporator. Final
traces of solvent were removed under vacuum for
overnight.

14.  The deposited lipid films were hydrated with buffer
(pH 6.5) by rotation at 60 rpm/min for 1 hr at the
corresponding temperature.
 The resulting vesicles were swollen for 2 hr at
room temperature.
 To prepare small vesicles, resulting LMVs were
sonicated at room temperature or 500˚C for 30 min
using a bath sonicator or probe sonicated at 40˚C
for 30 min.
 The sonicated vesicles were homogenized by
manual extrusion 10 times through a sandwich of
200 and 100 nm polycarbonate membrane.

15. Characterization
Vesicle size distribution and zeta potential
Vesicle size, size distribution and zeta potential were
determined by Dynamic Light Scattering Method.
 Vesicle morphology
Vesicle diameter can be determined using photon
correlation spectroscopy or dynamic light scattering (DLS)
method.
 Drug content
The drug content can be determined using one of the
instrumental analytical methods such as modified high
performance liquid chromatography method (HPLC)
method.

16.  Turbidity measurement
Turbidity of drug in aqueous solution can be measured
using nephelometer .
 Penetration ability
Penetration ability of Transfersomes can be evaluated
using fluorescence microscopy.
 Surface charge and charge density
Surface charge and charge density of transfersomes can
be determined using zetasizer.

17.  Degree of Deformability or Permeability Measurement
In the case of transfersomes, the permeability study is one of
the important and unique parameter for characterization. The
deformability study is done against the pure water as standard.
Transfersomes preparation is passed through a large number
of pores of known size. Particle size and size distributions are
noted after each pass by dynamic light scattering (DLS)
measurements.
 Entrapment Efficiency
The entrapment efficiency is expressed as the percentage
entrapment of the drug added. Entrapment efficiency was
determined by first separation of the unentrapped drug by use
of mini-column centrifugation method.
The entrapment efficiency is expressed as:
Entrapment efficiency= (amount entrapped/ total amount
added)*100.

18. Applications
 Transfersomes have the potential for the controlled
release of the administered drug and increasing the
stability of labile drugs due to the incorporation of
phospholipids.
 Large molecules weight compounds can be easily
transported across the skin with the help of
transfersomes. Eg- insulin, interferons.
 Transfersomes have been widely used as a carrier for
the transport of other proteins and peptides.
 Transfersomes obtain similar bioavailability to
subcutaneous injection. Human serum albumin was
found to be effective in producing the immune response

19.  Peripheral drug targeting: the ability of transferosomes
to target peripheral subcutaneous tissues is due to
minimum carrier associated drug clearance through
blood vessels in the subcutaneous tissue.
 Transferosomes improves the site specificity and
overall safety margin of corticosteroids which is
difficult to maintain by other routes.
 Transferosomes has also been used for the topical
analgesics, anaesthetic agents, anticancer, NSAIDs,
herbal drugs etc.

20. Examples
 Diractin ( ketoprofen in transferosome
gel) is used as an NSAID.

21. References
 Sachan R et al., Drug carrier transferosomes: A
novel tool for transdermal drug delivery system. Int
J R & D in Pharm Life Sciences. 2013.2,309-16.
 Kumavat SD et al., Transferosomes: A promising
approach for transdermal drug delivery system.
AJPSR. 2013. 3(5).
 Ravi K et al,. Transferosomes: A novel approach
for transdermal drug delivery. Int Res J Pharm.
2012. 20-24.
 Walve JR et al,. Transferosomes: A surrogated
carrier for transdermal drug delivery system.Int J
App Biology Pharma Tech. 2011.2(1)204-13.

22. Thank
you