不同促透剂对姜黄素凝胶体外透皮作用的影响

Influence of different penetration ehhancer on in vitro transdermal effect of curcumin gel

目的：制备姜黄素凝胶的外用制剂，考察不同促透剂对姜黄素凝胶的促透作用。方法：建立一种快速、灵敏的液质联用定量分析方法，以裸小鼠离体皮肤为渗透屏障，姜黄素为模型药物，Franz立式扩散法考察各处方姜黄素的体外透皮特性，计算各凝胶处方的累积渗透参数。结果：姜黄素分析方法的线性范围为10～800ng／ml，定量下限为10ng／ml；日内、日间精密度良好，RSD均〈15％；准确度符合要求。在1％的促透浓度下，6种促透剂对姜黄素的促透作用由强至弱依次为月桂氮革酮、N-甲基-2-吡咯烷酮、油酸、丙二醇、薄荷脑、卵磷脂。结论：姜黄素的HPLC—MS／MS分析方法符合要求，月桂氮革酮对姜黄素具有显著的促透作用。

Objective： To prepare curcumin gel with different penetration enhancer and study their skin permeation in vitro. Method： A rapid and sensitive HPLC-MS/MS quantitative method was established. Nude mouse skin was used as per- meation barrier and curcumin was selected as a model drug. Franz diffusion method was adopted to investigate the in vitro transdermal characteristics and the cumulative penetration parameters of each curcumin gel were calculated. Results： The cali- bration curve of curcumin had satisfactory linearity within the range of 10-800 ng/ml and the lower limit of quantitation was 10 ng/ml. The intra-day and inter-day RSD were ~15 %, and accuracy met the specified requirements. Under 1% penetration enhancing concentration, the penetration enhancing effects of 6 enhancers on curcumin were in sequence： azone, N-methyl-2- pyrrolidone,oleic acid, propylene glycol, menthol and lecithin. Conclusion： The HPLC-MS/MS method of curcumin met the requirements,azone had outstanding transdermal effect on curcumin gel.