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用于研究皮肤渗透促进剂作用的角质层脂质脂质体。

Stratum corneum lipid liposomes for investigating skin penetration enhancer effects.

作者信息

Bakonyi Mónika, Gácsi Attila, Berkó Szilvia, Kovács Anita, Csányi Erzsébet

机构信息

Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged Szeged H-6720 Hungary

出版信息

RSC Adv. 2018 Aug 2;8(48):27464-27469. doi: 10.1039/c8ra04129f. eCollection 2018 Jul 30.

Abstract

Knowledge of the mechanism of action of skin penetration enhancers is essential to formulators for optimizing formulations and to maximize the efficacy of enhancers. To obtain information about the effects of penetration enhancers as a fast initial screening, investigations have been performed to identify possible correlations of the biological effectiveness of penetration enhancers with their interaction with a well-defined model system consisting of skin mimic lipid bilayers, as determined by calcein release experiments using stratum corneum lipid liposomes (SCLLs). We aimed to investigate the enhancing effects of different concentrations of two chemical penetration enhancers, Kolliphor RH40 and Transcutol on SCLLs. The results obtained by SCLL-based techniques were compared with conventional penetration studies in case of Kolliphor RH40 to evaluate the potential of SCLLs as an alternative tool for screening various types and concentrations of penetration enhancers. As a result, calcein leakage assay performed with SCLL was considered to be a good model for the skin penetration enhancing effect. This method could be used as a time-saving and sensitive alternative screening technique in the early stage of the development of dermal formulations.

摘要

了解皮肤渗透促进剂的作用机制对于配方设计师优化配方以及最大化促进剂的功效至关重要。为了在快速初步筛选中获取有关渗透促进剂效果的信息,已开展研究,以确定渗透促进剂的生物学有效性与其与由皮肤模拟脂质双层组成的明确模型系统相互作用之间的可能关联,该关联通过使用角质层脂质脂质体(SCLLs)的钙黄绿素释放实验来确定。我们旨在研究两种化学渗透促进剂科利凡RH40和二甘醇单乙醚不同浓度对SCLLs的增强作用。对于科利凡RH40,将基于SCLL的技术获得的结果与传统渗透研究进行比较,以评估SCLLs作为筛选各种类型和浓度渗透促进剂的替代工具的潜力。结果,用SCLL进行的钙黄绿素泄漏测定被认为是皮肤渗透增强作用的良好模型。该方法可作为皮肤制剂开发早期节省时间且灵敏的替代筛选技术。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d45/9083441/31ac4bfb698a/c8ra04129f-f1.jpg

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