The effect of penetration enhancers on drug delivery through skin: a QSAR study

Ghafourian, Taravat and Zandasrar, Parinaz and Hamishekar, Hamed and Nokhodchi, Ali (2004) The effect of penetration enhancers on drug delivery through skin: a QSAR study. Journal of Controlled Release, 99 (1). pp. 113-125. ISSN 0168-3659. (The full text of this publication is not available from this repository)

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Abstract

Skin penetration enhancers are used to allow formulation of transdermal delivery systems for drugs that are otherwise insufficiently skin-permeable. A full understanding of the mode of action could be beneficial for the design of potent enhancers and for the choice of the enhancer to be used in the topical formulation of a special drug. In this study, the structural requirements of penetration enhancers have been investigated using the Quantitative Structure–Activity Relationship (QSAR) technique. Activities of naturally occurring terpenes, pyrrolidinone and N-acetylprolinate derivatives on the skin penetration of 5-fluorouracil, diclofenac sodium (DFS), hydrocortisone (HC), estradiol and benazepril have been considered. The resulting QSARs indicated that for 5-fluorouracil and diclofenac sodium, less hydrophobic enhancers were the most active. More precisely, molecular descriptors in the corresponding QSARs indicated the possible involvement of intermolecular electron donor–acceptor interactions. This was in contrast to the skin permeation promotion of hydrocortisone, estradiol and benazepril by enhancers, where a linear relationship between enhancement activity and n-octanol/water partition coefficients of enhancers was evident. The possible mechanisms of penetration enhancement as suggested by the QSARs will be discussed.

Item Type: Article
Uncontrolled keywords: skin absorption; QSAR; enhancer; transdermal penetration; transdermal permeation; permeation enhancer; penetration enhancer; hydrophobicity; lipophilicity
Subjects: Q Science
Q Science > QD Chemistry
Divisions: Faculties > Science Technology and Medical Studies > Medway School of Pharmacy
Depositing User: Taravat Ghafourian
Date Deposited: 23 Sep 2008 17:18
Last Modified: 20 May 2014 15:25
Resource URI: http://kar.kent.ac.uk/id/eprint/10416 (The current URI for this page, for reference purposes)
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