4.7 Article

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

Journal

PHARMACEUTICS
Volume 13, Issue 9, Pages -

Publisher

MDPI
DOI: 10.3390/pharmaceutics13091451

Keywords

alkanediols; preservation; triamcinolone acetonide; ex vivo skin penetration; stratum corneum lipids; confocal Raman spectroscopy (CRS)

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Alkanediols are found to enhance the skin penetration of triamcinolone acetonide, with the extent depending on the formulation used. Longer-chained alkanediols cause the lipids to convert to a more disordered state, favoring drug penetration. Conversely, shorter-chained alkanediols do not exhibit this behavior. Their penetration-enhancing effect is believed to be linked to an interaction with the hydrophilic regions of the stratum corneum.
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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