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生物基微乳剂使丙酸氯倍他索在皮肤长期滞留:一种治疗头皮银屑病的潜在工具。

Prolonged skin retention of clobetasol propionate by bio-based microemulsions: a potential tool for scalp psoriasis treatment.

作者信息

Langasco Rita, Tanrıverdi Sakine Tuncay, Özer Özgen, Roldo Marta, Cossu Massimo, Rassu Giovanna, Giunchedi Paolo, Gavini Elisabetta

机构信息

a Department of Chemistry and Pharmacy , University of Sassari , Sassari , Italy.

b Department of Pharmaceutical Technology, Faculty of Pharmacy , Ege University , Izmir , Turkey.

出版信息

Drug Dev Ind Pharm. 2018 Mar;44(3):398-406. doi: 10.1080/03639045.2017.1395458. Epub 2017 Nov 8.

DOI:10.1080/03639045.2017.1395458
PMID:29098874
Abstract

Novel effective and cosmetically acceptable formulations are needed for the treatment of scalp psoriasis, due to the poor efficacy of the current products. The challenge in developing safe, efficient, and convenient delivery systems for this drug was addressed in the present work by formulating clobetasol propionate-loaded W/O microemulsions (MEs). Pseudo-ternary phase diagrams were constructed by using a combination of biocompatible and biodegradable excipients. Characterization studies demonstrated that selected MEs had suitable technological features such as being Newtonian fluids, possessing low viscosity, and high thermodynamic stability. Photomicrographs showed a significant alteration of the skin structure after treatment with MEs, and a preferential concentration of these in the stratum corneum and epidermis. These data, together with ex vivo permeation results, suggested an enhanced topical targeted effect due to an increased drug retention efficacy in the upper skin layers, as desired. Moreover, the bio-based excipients selected could contribute to the healing of the psoriatic scalp. In this way, the improvement of clobetasol efficacy is combined with the useful properties of the microemulsion components and with environmental safety.

摘要

由于现有产品疗效不佳,因此需要新型有效的、在美容方面可接受的制剂来治疗头皮银屑病。在本研究中,通过配制负载丙酸氯倍他索的油包水微乳(MEs),解决了开发这种药物安全、高效且便捷的给药系统所面临的挑战。通过使用生物相容性和可生物降解的辅料组合构建了伪三元相图。表征研究表明,所选微乳具有合适的技术特性,如为牛顿流体、粘度低且热力学稳定性高。显微照片显示,微乳处理后皮肤结构发生了显著变化,且这些微乳在角质层和表皮中优先富集。这些数据与体外渗透结果一起表明,正如预期的那样,由于药物在上皮层中的保留效果增强,局部靶向作用得到了增强。此外,所选的生物基辅料有助于银屑病头皮的愈合。通过这种方式,丙酸氯倍他索疗效的提高与微乳成分的有益特性以及环境安全性相结合。

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