正极性驻极体和氮酮对环孢素A的体外透皮促渗作用

目的：研究正极性驻极体与不同浓度氮酮对环孢菌素A的经皮促渗作用，探索驻极体与化学促渗剂联合促渗的可行性及其协同促渗规律。方法：以环孢菌素A为模型药物，用电晕充电技术制备正极性驻极体，通过 Franz扩散池透皮实验和高效液相色谱技术研究正极性驻极体、不同浓度氮酮、正极性驻极体与不同浓度氮酮联用对环孢菌素A的体外促渗规律。结果：1）+500V , +1000V 和 +2000V 驻极体作用离体皮肤24h后，均对环孢菌素A具有较好的促渗效果；2）与对照组相比，1%氮酮、3%氮酮、5%氮酮分别作用于皮肤24h，对环孢菌素A的稳态透皮速率分别是对照组的6.72倍、2.11倍、1.43倍（P<0.05）；3）正极性驻极体与不同浓度的氮酮联合使用对环孢菌素A经皮促渗24h后，+1000V驻极体与1%氮酮联用组的促渗效果较好，但二者无叠加作用，即驻极体与不同浓度氮酮联用均没有表现出协同促渗作用。结论：正极性驻极体对环孢菌素A的经皮给药具有一定的促渗作用；正极性驻极体与氮酮联用对环孢菌素A未见协同促渗作用。

Promoting effect of positive polarity electret combined with azone on transdermal penetration of cyclosporin A

Objective To study the effects of positive polarity electret combined with different concentrations of azone in promoting the transdermal delivery of cyclosporin A,so as to explore the feasibility and the rule of electret combined with chemical enhancers in promoting transdermal delivery.Methods Cyclosporin A was used as the model drug in the present study.Positive polarity electret was prepared using corona charge technique.Franz diffusion cell system and HPLC techniques were applied to investigate the roles of positive polar electret,azone of different concentrations and their combination in promoting penetration of cyclosporin A in vitro. Results Satisfactory penetration promoting effects for cyclosporin A was observed in excised skin 24 h after exposure to +500 V,+1 000 V and +2 000 V electret.Compared to the control group,1%,3%,and 5% azone promoted the steady-state penetration rates of cyclosporin A by 6.72,2.11,and 1.43 folds after 24 h exposure.Combination of +1 000V electret plus 1% azone showed better penetration promoting effect than other combinations,but electret with different positive charges and different concentrations of azone showed no synergistic effect in promoting cyclosporin A penetration. Conclusion Positive polarity electret has a penetration promoting effect for transdermal delivery of cyclosporin A.Positive polarity electret and azone show no synergistic effect on promoting penetration of cyclosporin A.