黄芩苷壳聚糖微粒的构建及与乳膏体外经皮扩散行为的比较

目的:构建黄芩苷壳聚糖微粒,并与黄芩苷乳膏体外经皮扩散行为进行比较。方法:采用中和法构建微粒,正交试验法优化构建条件;利用Franz扩散池进行微粒与乳膏体外经皮扩散行为的比较。结果:微粒的最佳构建条件为:药物/材料比(1∶3),壳聚糖浓度2 mg/mL,反应10 min,包封率与载药量均达60%以上;微粒与乳膏经皮扩散36 h后,药物累积扩散百分率分别为4.04%和30%,皮层药物百分含量分别为0.11%和0.14%(n=3)且无统计学差异(W=7,P=0.127)。结论:采用中和法构建黄芩苷壳聚糖微粒,简便易行;且皮肤给药时具有局部药物贮库和一定的缓释的作用。

Construction on the Chitosan Microparticles of Baicalin and Comparison of Transdermal Diffusion in vitro of Baicalin in Chitosan Microparticles and Cream

Objective:To construct baicalin chitosan microparticles and compare the in vitro transdermal diffusion of baicalin in microparticles and cream.Methods:Baicalin chitosan microparticles were constructed by using neutralization method and optimized by orthogonal test;The in vitro transdermal diffusion of baicalin in microparticles and cream was compared by using Franz cell.Results:When the drug:stuff ratio was 1∶ 3,concentration of chitosan was 2 mg/mL,mixed duration was 10min,both the entrapment efficiency and drug loading efficiency of baicalin chitosan microparticles were over 60%;After 36 h,the cumulative release percentage of baicalin in microparticles and cream in vitro transdermal diffusion was 4.04% and 30%,respectively.The content of drug in microparticles and cream in the skin was 0.11% and 0.14%,respectively.And there was no significant difference(w=7,P=0.127)between the content of drug in microparticles and cream in the skin.Conclusion:The optimal procedure is simple and convenient with high entrapment efficiency and drug loading efficiency.The drug in the microparticles could be released slower and form local drug reservoir in the skin.