Chemical penetration enhancers in stratum corneum : Relation between molecular effects and barrier function

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Chemical penetration enhancers in stratum corneum : Relation between molecular effects and barrier function

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Publication Article, peer reviewed scientific
Title Chemical penetration enhancers in stratum corneum : Relation between molecular effects and barrier function
Author Quoc Dat Pham ; Björklund, Sebastian ; Engblom, Johan ; Topgaard, Daniel ; Sparr, Emma
Research Centre Biofilms - Research Center for Biointerfaces
Date 2016
English abstract
Skin is attractive for drug therapy because it offers an easily accessible route without first-pass metabolism. Transdermal drug delivery is also associated with high patient compliance and through the site of application, the drug delivery can be locally directed. However, to succeed with transdermal drug delivery it is often required to overcome the low permeability of the upper layer of the skin, the stratum corneum (SC). One common strategy is to employ so-called penetration enhancers that supposedly act to increase the drug passage across SC. Still, there is a lack of understanding of the molecular effects of so-called penetration enhancers on the skin barrier membrane, the SC. In this study, we provide a molecular characterization of how different classes of compounds, suggested as penetration enhancers, influence lipid and protein components in SC. The compounds investigated include monoterpenes, fatty acids, osmolytes, surfactant, and Azone. We employ natural abundance C-13 polarization transfer solid-state nuclear magnetic resonance (NMR) on intact porcine SC. With this method it is possible to detect small changes in the mobility of the minor fluid lipid and protein SC components, and simultaneously obtain information on the major fraction of solid SC components. The balance between fluid and solid components in the SC is essential to determine macroscopic material properties of the SC, including barrier and mechanical properties. We study SC at different hydration levels corresponding to SC in ambient air and under occlusion. The NMR studies are complemented with diffusion cell experiments that provide quantitative data on skin permeability when treated with different compounds. By correlating the effects on SC molecular components and SC barrier function, we aim at deepened understanding of diffusional transport in SC, and how this can be controlled, which can be utilized for optimal design of transdermal drug delivery formulations. (C) 2016 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY license.
DOI https://doi.org/10.1016/j.jconrel.2016.04.030 (link to publisher's fulltext.)
Link http://www.sciencedirect.com/science/article/pii/S0168365916302449 .Icon
Publisher Elsevier
Host/Issue Journal of Controlled Release;
Volume 232
ISSN 0168-3659
Pages 175-187
Language eng (iso)
Subject Keratin filament
Stratum corneum lipids
Monoterpene
Fatty acid
Solid-state NMR
Diffusion cell
Medicine
Research Subject Categories::PHARMACY
Handle http://hdl.handle.net/2043/23041 Permalink to this page
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