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亲脂性模型药物在水包油型微乳剂和两亲性乳膏中应用时的角质层渗透及定位比较。

Comparison of stratum corneum penetration and localization of a lipophilic model drug applied in an o/w microemulsion and an amphiphilic cream.

作者信息

Teichmann Alexa, Heuschkel Sandra, Jacobi Ute, Presse Gaëlle, Neubert Reinhard H H, Sterry Wolfram, Lademann Jürgen

机构信息

Department of Dermatology, Charité-Universitätsmedizin Berlin, Berlin, Germany.

出版信息

Eur J Pharm Biopharm. 2007 Nov;67(3):699-706. doi: 10.1016/j.ejpb.2007.04.006. Epub 2007 Apr 18.

Abstract

Vehicle dependent effects on the penetration behavior of drugs following topical application are well known from the literature. In this context, many reports concerning the enhancing activities for hydrophilic as well as lipophilic substances by colloidal drug carrier systems, particularly microemulsions, are available. However, there is little knowledge about the localization of the drugs within the skin and the stratum corneum, respectively. In the present study, the lipophilic dye curcumin incorporated in an oil-in-water microemulsion and in an amphiphilic cream was applied onto the skin of human volunteers. Using the method of tape stripping to remove the stratum corneum (SC), the depth profiles of the dye within the horny layer were compared. Applying the microemulsion, a deeper part of the SC was accessible by a number of 20 tapes removed and significantly smaller amounts of curcumin were found on the skin surface. Also differences in the distribution and localization of the dye within the stratum corneum were observed by laser scanning microscopy. Furthermore, curcumin was detected in hair follicles. It was obvious that the microemulsion led to a penetration into the complete follicular infundibula, whereas, following application of the cream, a fluorescence signal was only received from the follicular orifices.

摘要

文献中已充分了解到载体对局部应用药物渗透行为的影响。在此背景下,有许多关于胶体药物载体系统,特别是微乳剂对亲水性及亲脂性物质增强活性的报道。然而,对于药物在皮肤及角质层中的定位,人们了解甚少。在本研究中,将掺入水包油型微乳剂和两亲性乳膏中的亲脂性染料姜黄素应用于人类志愿者的皮肤。使用胶带剥离法去除角质层(SC),比较角质层中染料的深度分布。应用微乳剂时,通过去除20层胶带可接触到SC更深的部分,且在皮肤表面发现的姜黄素量显著更少。通过激光扫描显微镜还观察到染料在角质层中的分布和定位差异。此外,在毛囊中检测到了姜黄素。很明显,微乳剂可使其渗透到整个毛囊漏斗部,而应用乳膏后,仅从毛囊口接收到荧光信号。

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