化学促渗剂预处理与电致孔联用促进大鼠皮肤滞留环孢素A

Entrapment of cyclosporin A in rat skin during topical delivery by combination with chemical enhancers pretreatment and electroporation

目的:考察化学促渗剂预处理与电致孔联用对大鼠皮肤滞留环孢素A的促进作用。方法:使用化学促渗剂预处理大鼠皮肤2 h后,将含有0.5%环孢素A的40%乙醇混悬液应用于离体大鼠皮肤,同时在大鼠皮肤上施加电致孔。结果:氮酮和薄荷醇预处理皮肤和电致孔联用可明显提高环孢素A在大鼠表皮和真皮的滞留,与对照组相比,滞留量分别是对照组的10.4和11.7倍。结论:氮酮和薄荷醇预处理皮肤和电致孔联用具有协同作用,能够显著提高环孢素A在大鼠表皮和真皮中的滞留。

Objective： To investigate the entrapment of cyclosporin A in rat skin by combination with chemical enhancers pretreatment and electroporation. Methods： After skin pretreatment with chemical enhancers, and electroporation was applied. Results： The pretreatment with menthol or Azone following electroporation induced about 10-fold increase in the dermal delivery of cyclosporin A. Conclusion： The enhanced skin accumulation of cyclosporin A could help to significantly optimize the targeting of the drug without a concomitant increase of the systemic side effects.