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.
• Transferosomes are supramolecular entities that can pass through a
permeability barrier and thereby transport material from the application to
the destination.
• These are complex, vesicular aggregates optimized to attain flexible and
self-regulating membrane
4. COMPOSITION OF TRANSFEROSOME
• The transfersome is composed of two main aggregates namely,
• Firstly, an amphiphillic ingredient (phosphatidylcholine), in which the
aqueous solvents selfassembles into lipid bilayer that closes into a
simple lipid vesicle.
• Secondly, a bilayer softening component (such as a biocompatible
surfactant or amphiphile drug) that increases lipid bilayer flexibility
and permeability.
5. ADVANTAGE
• These shows greater permeation of the drugs through the skin
because of its flexible membranes.
• These serves as carrier for both small and large molecular weight
drugs.
• In Transfersomes, percentage of the drug entrapment is more.
• Protects the entrapped drug from atmospheric degradation.
• These are biocompatible and biodegradable.
• Site Specific therapy.
6. LIMITATION
• Transferosomes are chemically unstable because of their predisposition to
oxidative degradation.
• Purity of natural phospholipids is another criteria militating against
adoption of transferosomes as drug delivery vehicles.
• Transferosomes formulations and manufacturing aspects are expensive.
7. METHOD OF PREPARATION
The preparation methods of transfersomesare classified into the
following types:
• Film dispersion method
• Modified hand shaking method
8. Film dispersion method-
Film dispersion method is the one of the common preparation methods of
lipophilic drug transfersomes.
Thin film hydration technique is employed for the preparation of
transfersomes which comprised three step-
1. A thin film is prepared from the mixture of vesicles forming ingredients that is
phospholipids and surfactant by dissolving in a volatile organic solvent
(chloroform-methanol). Organic solvent is then evaporated using rotary
evaporator. Final traces of solvent were removed under vacuum for overnight.
2. A prepared thin film is hydrated with buffer (pH 6.5) by rotation at 60 rpm for
1 hr at the corresponding temperature. The resulting vesicles were swollen for 2
h at room temperature.
3. To prepare small vesicles, resulting vesicles were sonicated at room
temperature or 50°C for 30 min using a bath sonicator or probe sonicatedat 4°C
for 30 min. The sonicated vesicles were homogenized by manual extrusion 10
times through a sandwich of 200 and 100 nm polycarbonate membranes.
9. Modified handshaking method-
• Drug, lecithin (PC), and edge activator were dissolved in
ethanol:chloroform(1:1) mixture.
• Organic solvent was removed by evaporation while handshaking
above lipid transition temperature (43°C). A thin lipid film was formed
inside the flask wall with rotation. The thin film was kept overnight for
complete evaporation of solvent.
• The film was then hydrated with phosphate buffer (pH 7.4) with
gentle shaking for 15 min at corresponding temperature. The
transfersome suspension further hydrated up to 1 h at 2-8°C.
10.
11. Parameters Evaluation test
Vesicle size distribution and zeta potential Dynamic light scattering method
Vesicle morphology Dynamic light scattering method and
photon correlation spectroscopy
Drug content Analysis by help of HPLC
Turbidity measurement Neplometer
Penetration ability Flourescence microscopy
Surface charge and charge density Zeta sizer
Entrapment efficiency (amount of drug entrapped/total amount
of drug) * 100
CHARACTERIZATION
12. APPLICATION
• 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.
• 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.