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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 transdermal effect of positive electrets and different concentrations of azone on cyclosporin A (CsA) and to explore the feasibility of synergistic enhancement of electret and chemical penetration enhancers law. Methods CsA was used as a model drug to prepare a positive electrette by corona charging. The Franz diffusion cell transdermal test and high performance liquid chromatography (HPLC) were used to study the effects of electret with different surface potentials, azone at different concentrations, CsA in vitro with the role of promoting permeability. Results CsA had a good effect on the exfoliation of +5 000 V, +1 000 V and +2 000 V elevations on exfoliated skin, while 1%, 3% and 5% Azone acted on the skin respectively After 24 h, the steady-state transdermal rate of CsA was 6.72, 2.11 and 1.43 times higher than that of the blank control group respectively. When the positive electrets with different surface potentials were combined with Azone at different concentrations for 24 h, The combination of +1000 V electret and 1% Azone showed better promoting effect. However, the combination of positive electrets with different surface potentials and different concentrations of Azone did not show synergistic effect. Conclusion The positive electrets have a certain effect on the transdermal delivery of CsA. The combination of positive electrets and azone does not show a synergistic effect on CsA.