School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 807, Taiwan, ROC.
Department of Neurology, China Medical University Hospital, Yuh-Der Road, Taichung City 404, Taiwan, ROC; School of Medicine, Medical College, China Medical University, Taichung City 404, Taiwan, ROC.
Colloids Surf B Biointerfaces. 2018 Jan 1;161:121-128. doi: 10.1016/j.colsurfb.2017.10.015. Epub 2017 Oct 10.
The aim of the present study was to design a microemulsion for catechin topical application. A mixture experimental design with five independent variables (X: oil, X: surfactant, X: catechin, X: cosurfactant and X: water) was developed, and the response surface methodology was used to study the effect of formulation components on physiochemical characteristics and penetration capacity of a catechin-loaded microemulsion, and to obtain an optimal microemulsion formulation. The results showed that the drug-loaded microemulsion formation and characteristics were related to many parameters of the components. The transdermal amounts in receiver cells and skin deposition amount remarkably increased about 4.1-111.6-fold and 0.6-7.6-fold respectively. The lag time was significantly shortened from 10h to 1.0-6.7h. The optimal formulation with 20% surfactant, 30% cosurfactant and 2.6% Catechin was subjected to stability and irritation tests. The results showed that the physicochemical characteristics and catechin level of the drug-loaded microemulsion did not show significant degradation after 3 months of storage at 25°C.The catechin-loaded microemulsion did not cause significant irritation compared to the water-treated group.
本研究旨在设计一种用于儿茶素局部应用的微乳。采用五因素混合实验设计(X:油,X:表面活性剂,X:儿茶素,X:助表面活性剂和 X:水),并使用响应面法研究配方成分对载药微乳的理化特性和渗透能力的影响,以获得最佳的微乳配方。结果表明,载药微乳的形成和特性与各成分的许多参数有关。在接受细胞中的透皮量和皮肤沉积量分别显著增加了约 4.1-111.6 倍和 0.6-7.6 倍。滞后时间从 10h 显著缩短至 1.0-6.7h。将最佳配方(20%表面活性剂、30%助表面活性剂和 2.6%儿茶素)进行稳定性和刺激性试验。结果表明,载药微乳在 25°C 下储存 3 个月后,其理化特性和儿茶素水平没有明显降解。与水治疗组相比,载药微乳没有引起明显的刺激。