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A water gradient can be used to regulate drug transport across skin

Björklund, Sebastian LU ; Engblom, Johan; Thuresson, Krister LU and Sparr, Emma LU (2010) In Journal of Controlled Release 143(2). p.191-200
Abstract
At normal conditions there is a substantial water gradient over the skin as it separates the water-rich inside of the body from the dry outside. This leads to a variation in the degree of hydration from the inside to the outside of skin and changes in this gradient may affect the structure and function of skin. In this study we raise the question: How do changes in the water gradient across skin affect its permeability? We approach this problem in novel diffusion experiments that permit strict control of the gradient in the chemical potential of water and hence well-defined boundary conditions. The results demonstrate that a water gradient can be used to regulate transport of drugs with different lipophilic characteristics across the skin... (More)
At normal conditions there is a substantial water gradient over the skin as it separates the water-rich inside of the body from the dry outside. This leads to a variation in the degree of hydration from the inside to the outside of skin and changes in this gradient may affect the structure and function of skin. In this study we raise the question: How do changes in the water gradient across skin affect its permeability? We approach this problem in novel diffusion experiments that permit strict control of the gradient in the chemical potential of water and hence well-defined boundary conditions. The results demonstrate that a water gradient can be used to regulate transport of drugs with different lipophilic characteristics across the skin barrier. It is shown that the transport of metronidazole (log P(o/w)=0.0) and methyl salicylate (log P(o/w)=2.5) across skin increases abruptly at low water gradients, corresponding to high degrees of skin hydration, and that this effect is reversible. This phenomenon is highly relevant to drug delivery applications due to its potential of temporarily open the skin barrier for transdermal drug delivery and subsequently close the barrier after treatment. Further, the results contribute to the understanding of the occlusion effect and indicate the boundary conditions of the water gradient needed to make use of this effect. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Controlled Release
volume
143
issue
2
pages
191 - 200
publisher
Elsevier
external identifiers
  • wos:000277219200005
  • pmid:20074596
  • scopus:77950341634
ISSN
1873-4995
DOI
10.1016/j.jconrel.2010.01.005
language
English
LU publication?
yes
id
a30a1399-8042-48ae-99ca-39ad1583cce1 (old id 1541054)
date added to LUP
2010-02-02 14:47:21
date last changed
2018-07-15 03:15:49
@article{a30a1399-8042-48ae-99ca-39ad1583cce1,
  abstract     = {At normal conditions there is a substantial water gradient over the skin as it separates the water-rich inside of the body from the dry outside. This leads to a variation in the degree of hydration from the inside to the outside of skin and changes in this gradient may affect the structure and function of skin. In this study we raise the question: How do changes in the water gradient across skin affect its permeability? We approach this problem in novel diffusion experiments that permit strict control of the gradient in the chemical potential of water and hence well-defined boundary conditions. The results demonstrate that a water gradient can be used to regulate transport of drugs with different lipophilic characteristics across the skin barrier. It is shown that the transport of metronidazole (log P(o/w)=0.0) and methyl salicylate (log P(o/w)=2.5) across skin increases abruptly at low water gradients, corresponding to high degrees of skin hydration, and that this effect is reversible. This phenomenon is highly relevant to drug delivery applications due to its potential of temporarily open the skin barrier for transdermal drug delivery and subsequently close the barrier after treatment. Further, the results contribute to the understanding of the occlusion effect and indicate the boundary conditions of the water gradient needed to make use of this effect.},
  author       = {Björklund, Sebastian and Engblom, Johan and Thuresson, Krister and Sparr, Emma},
  issn         = {1873-4995},
  language     = {eng},
  number       = {2},
  pages        = {191--200},
  publisher    = {Elsevier},
  series       = {Journal of Controlled Release},
  title        = {A water gradient can be used to regulate drug transport across skin},
  url          = {http://dx.doi.org/10.1016/j.jconrel.2010.01.005},
  volume       = {143},
  year         = {2010},
}