正极性驻极体和氮酮对环孢素A的体外透皮促渗作用  

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

作　　者：梁媛媛[1] 马琳[1] 崔黎丽[2] 董法杰[1] 刘鸿越[2] 郭鑫[1] 江键[1] 

机构地区：[1]第二军医大学基础部数理教研室,上海200433 [2]第二军医大学药学院无机化学教研室,上海200433

出　　处：《第二军医大学学报》2012年第6期617-620,共4页Academic Journal of Second Military Medical University

基　　金：国家自然科学基金(50577066;50977089);上海市自然科学基金(10ZR1437600)~~

摘　　要：目的研究正极性驻极体与不同浓度氮酮对环孢素A(cyclosporin A,CsA)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CsA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不同表面电位正极性驻极体、不同浓度氮酮及两者联用对CsA的体外促渗作用。结果+500 V、+1 000 V和+2 000 V驻极体作用离体皮肤24 h后,均对CsA具有较好的促渗效果;1%、3%、5%氮酮分别作用于皮肤24 h后,对CsA的稳态透皮速率分别是空白对照组的6.72、2.11、1.43倍;不同表面电位正极性驻极体与不同浓度的氮酮联合使用对CsA经皮作用24 h后,+1 000 V驻极体与1%氮酮联用组的促渗效果较好,但不同表面电位的正极性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CsA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CsA未见协同促渗作用。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.

关 键 词：驻极体 氮酮 环孢素A 皮肤投药 

分 类 号：R943.43[医药卫生—药剂学]