青藤碱微乳体外透皮特性的研究

Transdermal delivery character of sinomenine microemulsion

目的:制备青藤碱微乳,研究青藤碱微乳及透皮吸收促进剂对体外透皮吸收的影响。方法:Zetasize多功能电位/粒度分析仪测定青藤碱微乳的粒度及其分布。用稳定性实验考察青藤碱微乳的稳定性。用Valia-Chien扩散池,研究青藤碱微乳的透皮速率以及薄荷脑、冰片、肉豆蔻酸异丙酯(IPM)等透皮促进剂对青藤碱微乳吸收的影响。结果:青藤碱微乳液滴的平均粒径均为31.3 nm。青藤碱微乳具有很好的稳定性。青藤碱微乳的平均透皮速率为(32.238±1.13)μg/cm2.h,几种促进剂对青藤碱微乳经皮渗透都有显著的促进作用(P<0.05)。以含2%冰片组促渗效果最好。结论:所制备的微乳具有很好的透皮速率,有望成为青藤碱的新型经皮给药制剂,薄荷脑、冰片和肉豆蔻酸异丙酯可以作为促渗剂用于青藤碱经皮吸收制剂。

AIM： To prepare O/W microemulsion formulation containing sinomenine and investigate the effect of different penetration enhancers on transermal delivery character of microemulsion in vitro. METHODS： The microemulsions were prepared and characterized using Zetasize potential/particle size analysis instrument. The stability tests were performed to evaluate the sinomenine microemulsions. Franz diffusion cell was adopted as the apparatus for in vitro transdermal test. Excised Wistar-rat abdomen skin was pretreated with penetration enhancers, such as menthol, borneol and isopropyl myristate. RESULTS： The average droplet size of the microemulsion was about 31.3 nm. A high permeation rate of （32. 238 ± 1.13 ） μg/cm^2 · h was showed in vitro. All the enhancers showed significant enhancement effect on the transdermal behavior of sinomenine microemulsion. 2% borneol had the strongest effect in all. CONCLUSION： These results indicate that the studied microemulsion system with high permeation rate may be a promising vehicle for the transdermal delivery of sinomenine. Menthol, borneol and isopropyl myristate were found to be the proper penetration enhancers in the transdermal preparation.