目的 考察苦参碱传递体对大鼠经皮给药后皮肤局部药物质量浓度经时变化，评价其透皮释药性能。方法 大鼠腹部脱毛，以非封闭方式经皮给予苦参碱传递体混悬液，应用微透析采样技术，结合RP-HPLC法，测定皮肤透析液中的药物质量浓度；比较苦参碱传递体及其脂质体、水溶液（含0.8%去氧胆酸钠）经皮给药后大鼠皮肤透析液中药物质量浓度经时曲线的差异。结果 苦参碱传递体给药后透析液中药物质量浓度达峰时间（t_max）为（4.200±0.447）h，最大药物浓度（C_max）为（0.927±0.251）μg/mL，药时曲线下面积（AUC_0-8）为（5.033±1.526）μg?h?mL^?1。苦参碱传递体的C_max和AUC_0-8显著高于其脂质体和水溶液（含0.8%去氧胆酸钠），而t_max较后两者显著减小（P＜0.05）。结论 在体皮肤微透析可用于苦参碱传递体的透皮释药性能评价；苦参碱传递体具有透皮快、渗透量高等特点。

Objective To investigate the changes of matrine concentration in rat local skin with time after transdermal administration of matrine transfersomes, and to evaluate the transdermal delivery properties. Methods The matrine transfersomes were applied non-occlusively onto rat skin in vivo with abdominal hair removal, and the concentration of drugs in microdialysate of skin was detected by microdialysis and reverse phase high performance liquid chromatography. Furthermore, the concentration-time curves of matrine in microdialysates of skin were compared among marine transfersomes, liposomes, and deoxysodium cholate solution. Results After the transfersomes were given to rats, the maximum peak time (t_max) of matrine skin concentration appeared at (4.200 ± 0.447) h. The maximum skin concentration (C_max) was (0.927 ± 0.251) μg/mL and area under the curve (AUC_0-8) was (5.033 ± 1.526) μg?h?mL^?1, which were much higher than those of the liposomes and the solution (containing 0.8% sodium deoxycholate, P < 0.05), while t_max shortened much more than that of them. Conclusion In vivo skin microdialysis could be used to assess the transdermal delivery properties of matrine transfersomes. And matrine transfersomes have the good transdermal permeability and efficacy.

宁夏回族自治区科技攻关计划项目（201087）