熊果酸纳米混悬凝胶剂的制备及其体外透皮研究

目的 制备熊果酸纳米混悬凝胶剂(UA-NS-gel),并考察其体外透皮性能.方法 采用反溶剂沉淀联合高压均质法制备UA-NS,再以卡波姆940为基质制成凝胶剂(UA-NS-gel);采用Franz扩散池法进行体外透皮试验,比较UA-NS-gel和熊果酸凝胶剂(UA-gel)的体外经皮渗透量及滞留量.结果 UA-NS-gel 24 h药物经皮渗透量为(104.40±6.48)μg/cm2,明显高于UA-gel的(28.56±2.16)μg/cm2 (P<0.01);UA-NS-gel皮肤滞留量为(138.08±19.39)μg/cm2,高于UA-gel的(70.51±14.77)μg/cm2 (P<0.05).结论 将熊果酸制成纳米混悬凝胶剂,能够有效地增加药物的皮肤渗透性能和皮肤的滞留量.

Study on preparation and in vitro transdermal penetration of nanosuspension-based gel of ursolic acid

Objective To prepare a nanosuspensions-based gel of ursolic acid (UA-NS-gel)and investigate the in vitro transdermal penetration characteristics.Methods UA-NS was prepared by anti-solvent precipitation and high pressure homogenization method and then transformed into gel with carbopol 940 as support base.The cumulative permeation amount and the amount of drug in the skin of UA-NS-gel were assessed by Franz-diffiusion and compared with UA conventional hydrogel (UA-gel).Results The amount of UA permeated through the skin and in the skin after applying UA-NS-gel for 24 h were (104.40±6.48) μg/cm2 and (138.08±19.39) μg/cm2,which were significantly higher than UA-gel of (28.56±2.16) μg/cm2 (P<0.01) and (70.51±14.77) μg/cm2 (P<0.05),repectively.Conclusion The UA-NS-gel has the ability to increase the transdermal penetration and drug concentration in the skin.