芍药苷凝胶剂与醇质体凝胶剂透皮性能比较

Comparison on Transdermal Delivery of Paeoniflorin Gel and Paeoniflorin-ethosome Gel

摘要:

目的：比较芍药苷凝胶剂与芍药苷醇质体凝胶剂的体外透皮性能，判断芍药苷的透皮形式。方法：采用改良Franz扩散池法，以大鼠腹皮为体外模型，考察芍药苷凝胶剂与芍药苷醇质体凝胶剂中芍药苷的透皮速率及滞留量。运用HPLC测定透皮液中芍药苷含量，流动相乙腈-0.4%冰乙酸溶液（14：86），检测波长230 nm。结果：芍药苷醇质体凝胶剂中芍药苷的累计透过量（361.67±69.98）μg·cm^-2，14 h累计透过率（17.42±3.34）%，分别为芍药苷凝胶剂的1.76倍和2.03倍。芍药苷在凝胶剂和醇质体凝胶剂中的透过方式均符合零级方程；在透皮时部分醇质体以完整形式透过皮肤。结论：醇质体载药体系通过变形性及与皮肤的融合性提高了芍药苷的经皮渗透性。

Abstract:

Objective: The aim of this study was to investigate the penetration difference between paeoniflorin gel and paeoniflorin-ethosome gel after dermal application,and then identify the penetration form of paeoniflorin. Method: Improved Franz diffusion cell method were used in the transdermal delivery experiment with rat abdominal skin as in vitro model;and penetration rates,retention amounts on the dermal surface of paeoniflorin in two formulations were investigated.The amount of paeoniflorin in percutaneous receptor fluid and residual drugs were determined by HPLC. Result: The cumulative amount of penetration in paeoniflorin-ethosome gel was 1.76 times bigger than that in paeoniflorin gel and the percutaneous percent was 2.03 times bigger.Both percutaneous results were consistent with zero-level model.Parts of the paeoniflorin-ethosome permeated the skin was in an integrity structure. Conclusion: Because of its deformability and cutaneous integration,ethosome can enhance the permeability of paeoniflorin.