电致孔条件下秦艽水提液体内外透皮给药最优电学参数的研究

Optimal Electrical Parameters of Transdermal Delivery of Gentiana Aqueous Solution under the Electroporation Condition

目的探索电致孔条件下秦艽水提液体外透皮给药与体内透皮给药的最优电学参数并研究其相关性。方法采用双室扩散池,用电致孔导入仪产生多种电学参数条件,分别以离体和活体小鼠皮肤为透皮屏障进行秦艽药液电致孔条件下经皮渗透实验,以HPLC测定接收池中龙胆苦苷含量,确定最优的电学参数并考察其相关性。结果电致孔条件下秦艽水提液体外透皮给药的最优电学参数条件为脉冲电压300V、脉冲时间1.1ms、波形SW、脉冲频率140个·min-1、脉冲数300个;体内透皮给药的最优电学参数条件为脉冲电压300V、脉冲时间1.2ms、波形SW、脉冲频率140个·min-1、脉冲数300个,显示二者最优电学参数条件基本一致。结论电致孔条件下秦艽水提液体外透皮与体内透皮吸收之间相关性良好,故可利用体外实验研究药物的透皮规律,与此同时进行体内研究保证临床用药安全,为开发新型透皮给药系统提供了依据。

OBJECTIVE To explore the optimal electrical parameters of the transdermal delivery of Gentiana aqueous solution in vitro and in vivo under the electroporation condition,and to study its relevance. METHODS The electrical parameters were determined using the two-chambered diffusion cell and the electroporation equipment. The percutaneous penetration experiments on Gentiana aqueous solution were performed with the ex vivo and in vivo rat skin repectively the transdemal barrier. The content of gentiopicroside in the receiving pool was measured by HPLC and the optimal electrical parameters were determined. The relevance,and the content of lactate dehydrogenase in vitro and in vivo rat skin under the electroporation condition were detected. RESULTS Under the electroporation condition,the optimal electrical parameters in vitro transdermal delivery were as follows：pulse voltage 300 V,pulse duration 1.1 ms,waveform SW,pulse frequency 140 pulse·min-1,pulse number 300. The optimal conditions in vivo were as follows：pulse voltage 300 V,pulse duration 1.2 ms,waveform SW,pulse frequency 140 pulse·min-1,pulse number 300. The optimal electrical parameters of the two conditions were basically the same. CONCLUSION There was a good correlation between in vitro transdermal delivery and in vivo percutaneous absorption of Gentiana aqueous solution under the electroporation condition.