黄芩苷和牛血清白蛋白双缓释制剂的制备及释药性能检测

The dual release of baicalin and bovine serum albumin preparation and drug release performance testing

目的:将黄芩苷和牛血清白蛋白(bovine serum albumin,BSA)载入壳聚糖温敏凝胶,构建双缓释体系,检测凝胶对药物的体外释放情况。方法:采用乳化缩聚法制备黄芩苷-明胶微球(gelatin microspheres,GMS);用不同配比的壳聚糖溶液和β-甘油磷酸钠(β-glycerophosphate,β-GP)溶液制备壳聚糖温敏凝胶,观察在37℃的成胶情况,选择最佳配比;在此基础上,将不同浓度的黄芩苷-GMS与BSA共混于壳聚糖凝胶溶液,测定载药后的成胶情况及黄芩苷和BSA的体外释放情况。结果:成功制备了黄芩苷-GMS,载药率5.62%,包封率72.05%;1.8%壳聚糖溶液与9%的β-GP混合10min后可获得状态良好的凝胶;加载两种药物后的凝胶溶液相转变时间未发生改变;30d时低浓度组累积释放了63.79%,两个较高浓度组分别释放了74.86%、77.63%。结论:壳聚糖温敏凝胶可以同时负载黄芩苷-GMS和BSA两种药物,在室温下呈溶液状态,37℃下经过10min可转变成半固体凝胶,在体外释药可达30d。黄芩苷和牛血清白蛋白双缓释制剂的制备和释药性能检测为牙周组织修复再生药物的研制提供了基础。

Objective：To prepare chitosan thermosensitive hydrogel for slow release both baicalin and bovine serum albumin （BSA） ,and to observe the release properties vitro. Methods ：The baicalin-gelatin microspheres （GMS） were prepared by chemical emulsion polycondensation. The chitosan thermosensitive hydrogel system was prepared by using different proportions of chitosan solution and 13-GP,observed gelation at 37℃ ,and selected the best ratio. On this basis, the different concentrations of baicalin-GMS and BSA were incorporated into the chitosan thermosensitive hydrogel system. Results： Baicalin-GMS were prepared successfully,and the rate of drug loading and encapsulation efficiency was respectively 5.62% and 72. 05%. The ideal state of the gel was formed by 1.8% chitosan solution and 9% after 10 rain. When two drugs were incorporated into chitosan thermosensitive hydrgel,There was no apparent change in the time of phase transition of gel solution. The low concentration group cumulative release was 63.79% afer 30 days and the two higher concentrations were released 74.86% ,77.63%. Conclusions：Chitosan thermosensitive hydrogel system can simultaneously loaded baicalin-GMS and BSA,melt at room temperature. It can be trans- formed into semi-solid gel at 37℃ after 10 min,and drug release up to more than 30 d in vitro.