用电致孔法促进环孢素A的皮肤滞留

目的研究致孔电压、致孔时间及脉冲模式对环孢素A在大鼠皮肤各层中滞留的影响。方法将质量分数为0.5%的环孢素A的乙醇(体积分数为40%)混悬液应用于离体大鼠皮肤,同时在大鼠皮肤施加电致孔。实验结束后,用胶带剥离法分离角质层,HPLC法测定角质层和大鼠去角质层皮肤及接受液中的药物含量。结果大鼠表皮和真皮中环孢素A的含量随致孔电压的升高略有增加,随致孔时间的增加而增加,使用3次/min的脉冲模式大鼠去角质层中的药物滞留量最多,并且使用电致孔这一物理促渗法未显著增加接受液中环孢素A的含量。结论电致孔法能够提高环孢素A皮肤局部用药效果,从而减少药物体循环带来的不良反应。

Investigation into the potential of electroporation facilitated entrapment of cyclosporin A in skin

Objective To investigate the entrapment of cyclosporin A in rat skin by electroporation.Methods A suspension of 0.5 %(w) cyclosporin A,which was prepared from normal saline containing 40% ethanol,was applied onto the rat skin.The drug concentrations in the skin and receiver medium were determined by HPLC.Results With an increase of pulse voltage,the drug deposited in the deeper skin was moderate enhanced.As the pulse time increased,the drug retained in the deeper skin was slightly augmented.The pulse rate of 3 times per min was chosen and the higher permeation of the drug into the deeper skin was obtained.At the same time,the amount of cyclosporin A in the receiver medium was not obviously enhanced compared to the control.Conclusion The electroporation method can enhance the local effect of cyclosporin A without the increase of systemic side effects.