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

Ghafourian, Taravat, Zandasrar, Parinaz, Hamishekar, Hamed, 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. (doi:10.1016/j.jconrel.2004.06.010) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:10416)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided.
Official URL:
https://doi.org/10.1016/j.jconrel.2004.06.010

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
DOI/Identification number: 10.1016/j.jconrel.2004.06.010
Uncontrolled keywords: skin absorption; QSAR; enhancer; transdermal penetration; transdermal permeation; permeation enhancer; penetration enhancer; hydrophobicity; lipophilicity
Subjects: Q Science
Q Science > QD Chemistry
Divisions: Divisions > Division of Natural Sciences > Medway School of Pharmacy
Depositing User: Taravat Ghafourian
Date Deposited: 23 Sep 2008 17:18 UTC
Last Modified: 16 Nov 2021 09:49 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/10416 (The current URI for this page, for reference purposes)

University of Kent Author Information

Ghafourian, Taravat.

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Nokhodchi, Ali.

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