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Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration
Pharmaceutics ( IF 5.4 ) Pub Date : 2021-09-11 , DOI: 10.3390/pharmaceutics13091451
Melanie Sigg 1 , Rolf Daniels 1
Affiliation  

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.

中文翻译:

烷二醇对角质层脂质和曲安奈德皮肤渗透的影响

烷二醇广泛用作皮肤制剂中的多功能成分。除了它们的防腐作用外,考虑到它们对药物渗透的可能影响对于它们的使用也是必不可少的。在本研究中,研究了 2-甲基-2,4-戊二醇、1,2-戊二醇、1,2-己二醇和 1,2-辛二醇对来自四种不同半固体制剂的曲安奈德皮肤渗透的影响。此外,进行共焦拉曼光谱测量以检查烷二醇对角质层脂质含量和顺序的影响。发现烷二醇增加曲安奈德的渗透。然而,程度在很大程度上取决于所使用的配方。在某些配方中,1,2-戊二醇表现出最高的效果,而在其他情况下,渗透增强效果随着所用烷二醇的烷基链长度而增加。所测试的链烷二醇均未从角质层中提取脂质,也未降低其厚度。尽管如此,长链烷二醇会导致脂质转化为更无序的状态,这有利于药物渗透。对于较短链的烷二醇,无法检测到这种行为。因此,它们的渗透增强作用应该与角质层亲水区域的相互作用有关。这有利于药物渗透。对于较短链的烷二醇,无法检测到这种行为。因此,它们的渗透增强作用应该与角质层亲水区域的相互作用有关。这有利于药物渗透。对于较短链的烷二醇,无法检测到这种行为。因此,它们的渗透增强作用应该与角质层亲水区域的相互作用有关。
更新日期:2021-09-12
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