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Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration

Alkanediols are widely used as multifunctional ingredients in dermal formulations. In addition to their preservative effect, considering their possible impact on drug penetration is also essential for their use. In the present study, the influence of 2-methyl-2,4-pentanediol, 1,2-pentanediol, 1,2-he...

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Autores principales: Sigg, Melanie, Daniels, Rolf
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8469070/
https://www.ncbi.nlm.nih.gov/pubmed/34575527
http://dx.doi.org/10.3390/pharmaceutics13091451
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author Sigg, Melanie
Daniels, Rolf
author_facet Sigg, Melanie
Daniels, Rolf
author_sort Sigg, Melanie
collection PubMed
description Alkanediols are widely used as multifunctional ingredients in dermal formulations. In addition to their preservative effect, considering their possible impact on drug penetration is also essential for their use. In the present study, the influence of 2-methyl-2,4-pentanediol, 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol on the skin penetration of triamcinolone acetonide from four different semisolid formulations was investigated. Furthermore, confocal Raman spectroscopy measurements were performed to examine the influence of the alkanediols on stratum corneum lipid content and order. Alkanediols were found to increase the penetration of triamcinolone acetonide. However, the extent depends strongly on the formulation used. In certain formulations, 1,2-pentanediol showed the highest effect, while in others the penetration-enhancing effect increased with the alkyl chain length of the alkanediol used. None of the tested alkanediols extracted lipids from the stratum corneum nor reduced its thickness. Notwithstanding the above, the longer-chained alkanediols cause the lipids to be converted to a more disordered state, which favors drug penetration. This behavior could not be detected for the shorter-chained alkanediols. Therefore, their penetration-enhancing effect is supposed to be related to an interaction with the hydrophilic regions of the stratum corneum.
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spelling pubmed-84690702021-09-27 Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration Sigg, Melanie Daniels, Rolf Pharmaceutics Article Alkanediols are widely used as multifunctional ingredients in dermal formulations. In addition to their preservative effect, considering their possible impact on drug penetration is also essential for their use. In the present study, the influence of 2-methyl-2,4-pentanediol, 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol on the skin penetration of triamcinolone acetonide from four different semisolid formulations was investigated. Furthermore, confocal Raman spectroscopy measurements were performed to examine the influence of the alkanediols on stratum corneum lipid content and order. Alkanediols were found to increase the penetration of triamcinolone acetonide. However, the extent depends strongly on the formulation used. In certain formulations, 1,2-pentanediol showed the highest effect, while in others the penetration-enhancing effect increased with the alkyl chain length of the alkanediol used. None of the tested alkanediols extracted lipids from the stratum corneum nor reduced its thickness. Notwithstanding the above, the longer-chained alkanediols cause the lipids to be converted to a more disordered state, which favors drug penetration. This behavior could not be detected for the shorter-chained alkanediols. Therefore, their penetration-enhancing effect is supposed to be related to an interaction with the hydrophilic regions of the stratum corneum. MDPI 2021-09-11 /pmc/articles/PMC8469070/ /pubmed/34575527 http://dx.doi.org/10.3390/pharmaceutics13091451 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sigg, Melanie
Daniels, Rolf
Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
title Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
title_full Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
title_fullStr Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
title_full_unstemmed Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
title_short Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
title_sort impact of alkanediols on stratum corneum lipids and triamcinolone acetonide skin penetration
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8469070/
https://www.ncbi.nlm.nih.gov/pubmed/34575527
http://dx.doi.org/10.3390/pharmaceutics13091451
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