柔性纳米脂质体作为环孢素经皮渗透载体的体外研究

 目的 研究柔性纳米脂质体对环孢素经皮渗透的促进作用。方法 采用改进的Franz扩散池体外经皮渗透实验技术，比较普通纳米脂质体、含有表面活性剂胆酸钠的柔性纳米脂质体以及胆酸钠胶团溶液对环孢素的经皮渗透促进作用。结果 将脂质体胶体溶液非封闭性应用于离体小鼠皮肤表面，柔性纳米脂质体促进药物穿透皮肤,8 h后皮肤药物的透过量为1.16μg·cm^-2,24 h后透过量达到1.88 μg·cm^-2，皮肤中药物残留量为(1.78±0.51)μg·cm^-2。普通纳米脂质体阻止药物透过皮肤却滞留药物于皮肤中,24 h后残留量为(0.72±0.19)μg·cm^-2。1%和40%胆酸钠溶液阻止药物进入皮肤。结论 柔性纳米脂质体具有促进药物经皮渗透而普通纳米脂质体具有滞留药物于皮肤中的作用，胆酸钠胶团阻止药物进入皮肤表面。

Flexible nano-liposomes as carriers for transdermal delivery of cyclosporine

OBJECTIVE To investigate the enhancing efffect of flexible nano-liposome on the transdermal delivery of cyclosporine.METHODS The effects of common nano-liposome,flexible nano-liposome containing sodium cholate and micelles on the penetration of cyclosporin A through excised mice skin were assessed by an in vitro permeation technique using modified Franz-diffusion cells.RESULTS When applied onto the mice skin non-occlusively,flexible nano-liposome promoted the transfer of cyclosporin A into the receiver.The permeation of cyclosporin A through per cm2 mice skin was 1.16 μg after 8h of transportation and amounted to 1.88 μg 24 h later.The residual amount in the skin was (1.78±0.51) μg·cm^-2.Common nano-liposome failed to transfer cyclosporin A into the receiver while promoted the accumulation of drug in the skin,up to (0.72±0.19) μg·cm^-2.1% and 40% Micelles precluded the transport of cyclosporin A into the mice skin.CONCLUSION Flexible nano-liposomes can be effective carriers for the transdermal delivery of cyclosporine.