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药物和化妆品活性成分透过人体角质层的渗透与扩散机制。

Mechanisms of penetration and diffusion of drugs and cosmetic actives across the human Stratum corneum.

作者信息

Neubert Reinhard H H

机构信息

Institute of Applied Dermatopharmacy at the Martin Luther University Halle-Wittenberg, Weinbergweg 23, 06120 Halle/Saale, Germany.

出版信息

Eur J Pharm Biopharm. 2024 Sep;202:114394. doi: 10.1016/j.ejpb.2024.114394. Epub 2024 Jul 6.

Abstract

Based on the structure of the Stratum corneum (SC) the potential penetration/diffusion pathways of drugs and cosmetic actives through the SC are presented and discussed. The well-known lipophilic pathway across the SC is presented and relevant examples are used to show that highly lipophilic molecules such as glucocorticoids, coenzyme Q10 etc. are accumulated in the SC and penetrate into the inner liquid like layer of the SC lipid bilayer by lateral diffusion. The diffusion into and across the SC of highly hydrophilic drugs and active substances such as urea, amino acids and peptides is still under discussion. Another diffusion pathway for the highly hydrophilic molecules via the corneocytes and the corneodesmosomes is presented and discussed, the corneocytary diffusion pathway.

摘要

基于角质层(SC)的结构,介绍并讨论了药物和化妆品活性成分通过SC的潜在渗透/扩散途径。介绍了穿过SC的著名亲脂性途径,并通过相关实例表明,糖皮质激素、辅酶Q10等高度亲脂性分子在SC中积累,并通过横向扩散渗透到SC脂质双层的内液样层中。尿素、氨基酸和肽等高度亲水性药物和活性物质进入和穿过SC的扩散仍在讨论中。提出并讨论了高度亲水性分子通过角质形成细胞和角质桥粒的另一种扩散途径,即角质形成细胞扩散途径。

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