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生物表面活性剂对氢化可的松皮肤渗透的影响。

Influence of Biosurfactants on Skin Permeation of Hydrocortisone.

作者信息

Abruzzo Angela, Parolin Carola, Corazza Elisa, Giordani Barbara, di Cagno Massimiliano Pio, Cerchiara Teresa, Bigucci Federica, Vitali Beatrice, Luppi Barbara

机构信息

Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.

Department of Pharmacy, Faculty of Mathematics and Natural Sciences, University of Oslo, Sem Sælands vei 3, 0371 Oslo, Norway.

出版信息

Pharmaceutics. 2021 May 31;13(6):820. doi: 10.3390/pharmaceutics13060820.

Abstract

One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by BC1 and BC9, on the skin permeation profile of hydrocortisone (HC, model drug). HC aqueous solubility and in vitro diffusion studies through porcine skin were performed in the presence of BC1-BS and BC9-BS at concentrations below and above critical micellar concentrations (CMC). Moreover, skin hydration tests and differential scanning calorimetry (DSC) analysis were performed to further investigate BS interaction with the outermost layer of the skin. Both BS increased HC solubility, especially at concentrations above their CMC. At concentrations below the CMC, drug permeation through the skin was improved, as the result of a dual effect: a) the formation of a superficial lipophilic environment, as confirmed by the reduction in skin hydration and b) the interaction between BS and the stratum corneum (SC), as demonstrated by the DSC curves. From the obtained data, it appears that BC1-BS and BC9-BS could represent new promising green excipients for drug permeation enhancement through the skin.

摘要

提高药物经皮扩散的最广泛使用的策略之一是使用渗透促进剂。这项工作的目的是研究由BC1和BC9产生的两种生物表面活性剂(BS)对氢化可的松(HC,模型药物)皮肤渗透曲线的影响。在低于和高于临界胶束浓度(CMC)的浓度下,在BC1-BS和BC9-BS存在的情况下进行了HC的水溶性和通过猪皮的体外扩散研究。此外,进行了皮肤水合测试和差示扫描量热法(DSC)分析,以进一步研究BS与皮肤最外层的相互作用。两种BS均增加了HC的溶解度,尤其是在高于其CMC的浓度下。在低于CMC的浓度下,药物经皮渗透得到改善,这是双重作用的结果:a)皮肤水合作用降低证实了表面亲脂性环境的形成,b)DSC曲线表明了BS与角质层(SC)之间的相互作用。从获得的数据来看,BC1-BS和BC9-BS似乎可能是用于增强药物经皮渗透的有前途的新型绿色辅料。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d90/8228446/5e0b1f8841b3/pharmaceutics-13-00820-g001a.jpg

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