传递体作为酮康唑经皮渗透载体的体外研究

Preparation and enhancement effect of ketoconazole transfersomes on transder-mal absorption

目的:制备酮康唑传递体,测定其含量;研究酮康唑传递体的经皮渗透促进作用。方法:用旋转蒸发法制备酮康唑传递体,反相HPLC法测定酮康唑的含量。采用改进的franz扩散池体外经皮渗透实验。以兔皮背部皮肤为透皮屏障,紫外分分光光度法测定普通纳米脂质体、含有表面活性剂胆酸钠酮康唑传递体(KCZ TF)、含3%的双戊烯(3%DP)和3%的氮酮(3%AZ)对酮康唑的促透效果。结果:制得酮康唑传递体。各种促进剂对酮康唑的促透效果顺序为:传递体> 3%双戊烯>3%氮酮>普通纳米脂质体。结论:实验证明,传递体对酮康唑具有良好的促透作用,与其它促透剂相比具有显著差异(P<0.05)或极显著的差异(P< 0.01)。

Objective： To prepare and determinate the ketoconazole（KCZ） transfersomes（TF） ,and to study the enhancing effect on the transdermal absorption of ketoconazole transfersomes. Methods： The rotary evaporation method was used for preparation of KCZ TF. The HPLC was employed in its determination. The excised rabbit skin was used as the percutaneous barrier, and the modified franz-diffusion cells were used in the test. The enhancement effect of common nano-liposome, transfersomes, 3% dipentene and 3% azone were compared in the transdermal absorption of ketoconazole. Results： The KCZ TF were prepared. The sequence of enhancement at difference transdermal enhancer are follows： transfersomes 〉 3% dipentene 〉 3% azone 〉 common nana-liposome. Conclusion ： It was showed that various transder enhancers could promote absorption of ketoconazole in different degrees and transfersomes was the most effective.