期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 60, 期 1, 页码 25-30出版社
ELSEVIER
DOI: 10.1016/j.ejpb.2004.12.003
关键词
monoolein; cyclosporin A; topical delivery; penetration enhancer; in vitro permeation
Topical delivery, of cyclosporin A (CysA) is of great interest for the treatment of autoimmune skin disorders, but it. is frequently ineffective due to poor drug penetration in the skin. The present study was aimed at investigating whether the presence of monoolein (a lipidic penetration enhancer) in a preparation of propylene glycol can improve CysA delivery to the skin. CysA was incorporated in a propylene glycol preparation containing 5-70% (w/w) of monoolein. The topical (to the skin) and transdermal (across the skin) delivery of CysA were evaluated in vitro using porcine ear skin mounted in a Franz diffusion cell. CysA was quantified by UV-HPLC. At 5%, monoolein increased only the transdermal delivery of CysA. At 10%, it increased both topical and transdermal delivery. When the concentration of monoolein was further increased (20-70% w/w), an interesting phenomenon was observed: the topical delivery of CysA was still elevated but its transdermal delivery was substantially reduced. It was concluded that monoolein (in propylene glycol formulations) can promote the, topical delivery of CysA with reduced transdermal delivery. (c) 2005 Elsevier B.V. All rights reserved.
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