Transfersomes are highly efficient edge activator (EA)-based ultraflexible vesicles
capable of, non-invasively, trespassing skin by virtue of their high, self-optimizing
deformability. This investigation presents different approaches for the optimization
of Transfersomes for enhanced transepidermal delivery of Diclofenac sodium (DS). Different
methods of preparation, drug and lipid concentrations and vesicle compositions were
employed, resulting in ultraflexible vesicles with diverse membrane characteristics.
Evaluation of Transfersomes was implemented in terms of their shapes, sizes, entrapment
efficiencies (EE%), relative deformabilities and in vitro skin permeation. Transfersomes
prepared with 95:5% (w/w) (PC:EA) ratio showed highest EE% (Span 85>Span 80>Na cholate>Na
deoxycholate>Tween 80). Whereas, those prepared using 85:15% (w/w) ratio showed highest
deformability (Tween 80 was superior to bile salts and spans). Transfersomes were
proved significantly superior in terms of, the amount of drug deposited in the skin
and the amount permeated, with an enhancement ratio of 2.45, when compared to a marketed
product. The study proved that the type and concentration of EA, as well as, the method
of preparation had great influences on the properties of Transfersomes. Hence, optimized
Transfersomes can significantly increase transepidermal flux and prolong the release
of DS, when applied non-occlusively.
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