萜烯类化合物对吲哚美辛脂质体凝胶透皮吸收的影响

Effects of terpenes on percutaneous absorption of indomethacin-loaded liposome gel

目的:制备吲哚美辛脂质体凝胶,考察不同吸收促进剂对其体外透皮吸收的影响。方法:以卡波姆作为凝胶基质,采用薄膜分散法制备脂质体,分别考察磷脂和胆固醇的比例、药物和磷脂的比例对吲哚美辛包封率的影响,优化并选择最佳处方;采用立式改良Franz扩散池,研究萜烯类化合物对吲哚美辛脂质体凝胶体外透皮吸收的影响。结果:磷脂/胆固醇(SPC/CH)及药物/磷脂的最佳比例分别为6∶1和1∶30。凝胶基质为4%卡波姆,最佳透皮吸收促进剂为2.5%葑酮,吲哚美辛脂质体凝胶的累积渗透量Q24达到(198.36±15.78)μg·cm^(-2),稳态透皮速率(JS)为(7.93±3.01)μg·cm^(-2)·h^(-1)。结论:2.5%葑酮对吲哚美辛脂质体凝胶的促渗作用良好,为今后开发经皮给药制剂提供理论基础。

Objective： To prepare indomethacin liposome gel and investigate the effects of different absorption enhancers on its percutaneous absorption in vitro. Methods： The indometbacin liposome gel was prepared by thin-film dispersion method with Carbomer gelling agents. The effects of the mass ratios of phospholipid/ cholesterol and drug/phospholipid on indomethacin entrapment efficiency were investigated to optimize and choose the best formulation. And the effect of terpenes penetration enhancers on transdermal permeation of the drug was evaluated using improved Franz diffusion cells. Results： The mass ratios of liquid/cholesterol and drug/liquid for the best formation were 6：1 and 1： 30, respectively. The preparation prepared using 4% Carbomer showed desirable characteristics and appearance. Indomethacin liposome gel using 2.5% fenchone showed the highest cumulative permeation amount （ Q24 ） of （ 198.36 ± 15.78 ） μg· cm ^-2 and fluxrate （Js） of （7.93 ± 3.01 ） μg· cm ^-2 · h^ -1 Conclusion： The highest eumulative permeation amount was obtained with fenchone 2.5% for indomethacin liposome gel. Indomethacin liposome gel has good potential for transdermal delivery.