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神经酰胺脂质体促进皮肤屏障恢复:一种基于天然皮肤脂质的新型制剂。

Ceramide liposomes for skin barrier recovery: A novel formulation based on natural skin lipids.

机构信息

University of Chemistry and Technology Prague, Faculty of Chemical Technology, Department of Organic Technology, Technická 5, 166 28 Prague, Czech Republic.

Institute of Macromolecular Chemistry of the Czech Academy of Sciences, Heyrovského nám. 2, 162 06 Prague 6, Czech Republic.

出版信息

Int J Pharm. 2021 Mar 1;596:120264. doi: 10.1016/j.ijpharm.2021.120264. Epub 2021 Jan 21.

DOI:10.1016/j.ijpharm.2021.120264
PMID:33486027
Abstract

Diseases related to a disrupted skin barrier are accompanied by lower levels of ceramides in the stratum corneum (SC) lipid matrix. Delivering ceramides directly into damaged skin is a viable alternative to conventional corticosteroids, but is hindered by their low skin bioavailability and limited nanoformulation ability. Here, we developed stable liposomal systems containing ceramides and other SC lipids, and tested their effectiveness in skin barrier repair. Lipid film hydration and high-pressure homogenization were used to prepare different types of liposomes. To determine the stability, the particle size and polydispersity index were measured. The optimal systems were found to include ceramide 3 and 6, cholesterol and stearic acid, with 10% urea in phosphate-buffered saline as the aqueous phase. The ability of the system to repair chemically-damaged porcine skin was tested. While treatment by a standard lipid suspension reduced the passage of a model permeant only to a limited extent, drug flux through the liposomally-treated skin was much closer to permeation through intact skin. The non-homogenized liposomes were more effective than their homogenized version. These findings were also confirmed by FTIR measurements. This suggests that our approach to liposomal development has considerable potential for the repair of a disrupted skin barrier.

摘要

与皮肤屏障破坏相关的疾病伴随着角质层(SC)脂质基质中神经酰胺水平降低。将神经酰胺直接递送至受损皮肤是替代传统皮质类固醇的可行方法,但由于其皮肤生物利用度低和纳米制剂能力有限而受到阻碍。在这里,我们开发了含有神经酰胺和其他 SC 脂质的稳定脂质体系统,并测试了它们在皮肤屏障修复中的有效性。脂质体薄膜水合作用和高压匀浆用于制备不同类型的脂质体。为了确定稳定性,测量了粒径和多分散指数。发现最佳系统包括神经酰胺 3 和 6、胆固醇和硬脂酸,以及磷酸盐缓冲盐水(PBS)中的 10%尿素作为水相。该系统修复化学损伤猪皮的能力进行了测试。虽然标准脂质混悬液的处理仅在一定程度上减少了模型渗透物的通过,但通过脂质体处理的皮肤的药物通量更接近完整皮肤的渗透。未经匀化的脂质体比匀化的脂质体更有效。这些发现也通过傅里叶变换红外光谱(FTIR)测量得到了证实。这表明我们的脂质体开发方法在修复受损皮肤屏障方面具有很大的潜力。

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