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The effects of polar excipients transcutol and dexpanthenol on molecular mobility, permeability, and electrical impedance of the skin barrier

Björklund, Sebastian LU ; Pham, Dat LU ; Jensen, Louise Bastholm; Knudsen, Nina Østergaard; Nielsen, Lars Dencker; Ekelund, Katarina; Ruzgas, Tautgirdas LU ; Engblom, Johan and Sparr, Emma LU (2016) In Journal of Colloid and Interface Science 479. p.207-220
Abstract

In the development of transdermal and topical products it is important to understand how formulation ingredients interact with the molecular components of the upper layer of the skin, the stratum corneum (SC), and thereby influence its macroscopic barrier properties. The aim here was to investigate the effect of two commonly used excipients, transcutol and dexpanthenol, on the molecular as well as the macroscopic properties of the skin membrane. Polarization transfer solid-state NMR methods were combined with steady-state flux and impedance spectroscopy measurements to investigate how these common excipients influence the molecular components of SC and its barrier function at strictly controlled hydration conditions in vitro with... (More)

In the development of transdermal and topical products it is important to understand how formulation ingredients interact with the molecular components of the upper layer of the skin, the stratum corneum (SC), and thereby influence its macroscopic barrier properties. The aim here was to investigate the effect of two commonly used excipients, transcutol and dexpanthenol, on the molecular as well as the macroscopic properties of the skin membrane. Polarization transfer solid-state NMR methods were combined with steady-state flux and impedance spectroscopy measurements to investigate how these common excipients influence the molecular components of SC and its barrier function at strictly controlled hydration conditions in vitro with excised porcine skin. The NMR results provide completely new molecular insight into how transcutol and dexpanthenol affect specific molecular segments of both SC lipids and proteins. The presence of transcutol or dexpanthenol in the formulation at fixed water activity results in increased effective skin permeability of the model drug metronidazole. Finally, impedance spectroscopy data show clear changes of the effective skin capacitance after treatment with transcutol or dexpanthenol. Based on the complementary data, we are able to draw direct links between effects on the molecular properties and on the macroscopic barrier function of the skin barrier under treatment with formulations containing transcutol or dexpanthenol.

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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Excipients, Molecular mobility, Skin permeability, Steady-state flux, Stratum corneum, Topical drug delivery
in
Journal of Colloid and Interface Science
volume
479
pages
14 pages
publisher
Elsevier
external identifiers
  • scopus:84992364610
  • wos:000380384700027
ISSN
0021-9797
DOI
10.1016/j.jcis.2016.06.054
language
English
LU publication?
yes
id
450f98c7-5745-4c02-b3d8-02c7a38bc18d
date added to LUP
2016-11-16 10:57:12
date last changed
2017-05-29 12:52:58
@article{450f98c7-5745-4c02-b3d8-02c7a38bc18d,
  abstract     = {<p>In the development of transdermal and topical products it is important to understand how formulation ingredients interact with the molecular components of the upper layer of the skin, the stratum corneum (SC), and thereby influence its macroscopic barrier properties. The aim here was to investigate the effect of two commonly used excipients, transcutol and dexpanthenol, on the molecular as well as the macroscopic properties of the skin membrane. Polarization transfer solid-state NMR methods were combined with steady-state flux and impedance spectroscopy measurements to investigate how these common excipients influence the molecular components of SC and its barrier function at strictly controlled hydration conditions in vitro with excised porcine skin. The NMR results provide completely new molecular insight into how transcutol and dexpanthenol affect specific molecular segments of both SC lipids and proteins. The presence of transcutol or dexpanthenol in the formulation at fixed water activity results in increased effective skin permeability of the model drug metronidazole. Finally, impedance spectroscopy data show clear changes of the effective skin capacitance after treatment with transcutol or dexpanthenol. Based on the complementary data, we are able to draw direct links between effects on the molecular properties and on the macroscopic barrier function of the skin barrier under treatment with formulations containing transcutol or dexpanthenol.</p>},
  author       = {Björklund, Sebastian and Pham, Dat and Jensen, Louise Bastholm and Knudsen, Nina Østergaard and Nielsen, Lars Dencker and Ekelund, Katarina and Ruzgas, Tautgirdas and Engblom, Johan and Sparr, Emma},
  issn         = {0021-9797},
  keyword      = {Excipients,Molecular mobility,Skin permeability,Steady-state flux,Stratum corneum,Topical drug delivery},
  language     = {eng},
  month        = {10},
  pages        = {207--220},
  publisher    = {Elsevier},
  series       = {Journal of Colloid and Interface Science},
  title        = {The effects of polar excipients transcutol and dexpanthenol on molecular mobility, permeability, and electrical impedance of the skin barrier},
  url          = {http://dx.doi.org/10.1016/j.jcis.2016.06.054},
  volume       = {479},
  year         = {2016},
}