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Role of edge activators and surface charge in developing ultradeformable vesicles with enhanced skin delivery

El Zaafarany, Ghada M., Awad, Gehanne A.S., Holayel, Samar M., Mortada, Nahed D.·2010·International Journal of Pharmaceutics
DOI 10.1016/j.ijpharm.2010.06.034
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Abstract

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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Metadata

Authors
El Zaafarany, G. M., Awad, G. A. S., Holayel, S. M., & Mortada, N. D.
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2010-09
Volume
397
Issue
1-2
Pages
164-172
ISSN
0378-5173
DOI
10.1016/j.ijpharm.2010.06.034
Cited by
485
References
0
Language
en
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)

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