雷公藤红素环糊精与油自组装小珠载药系统的制备及其体外评价

Preparation of self-assembled beads drug delivery system of tripterine based on cyclodextrin and oil as well as its in vitro evaluation

目的制备雷公藤红素环糊精与油自组装小珠,并对其进行体外评价。方法采用连续振摇法制备雷公藤红素自组装小珠,通过显微方法观察小珠的粒径和药物分布;差示扫描量热方法考察药物形态;HPLC法测定小珠的载药量和包封率;并对载药小珠体外释放度进行了测定。结果制得的载药小珠粒径(1.49±0.20)mm;载药量为(87.21±0.58)μg/g;包封率为(80.14±1.24)%。差示扫描量热表明药物以非晶形态存在。荧光标记后激光共聚焦显微镜观察显示,水难溶性药物主要分布在大豆油内核中。小珠在模拟肠液中6 h最大累积释药量可达80%。结论制备的自组装小珠载药系统工艺简单,是一种有发展潜力的适用于水难溶性中药的药物传递系统。

Objective To prepare the self-assembled beads drug delivery system of triptrine based on cyclodextrin and oil, and to carry out its in vitro evaluation. Methods The beads were prepared by a continuously shaking starting from a mixture ofcyclodextrin aqueous solution and oil. The bead diameter and drug distribution were investigated by microscopic observations, and drug disperse state was observed by differential scanning calorimetry （DSC）. The drug-loading and entrapment efficiency of tripterine in beads were investigated by HPLC. The in vitro dissolution of tripterine in beads was also determined. Results The diameter was in the range of （1.49± 0.20） mm. The drug-loading and encapsulation efficiency of the prepared beads were （87.21 ± 0.58） μg/g and （80.14 ± 1.24）%, respectively. DSC suggested that tripterine existed as amorphous form in beads. Confocal microcopy showed that the hydrophobic drug was localized inside the beads. The maximum cumulative release amount oftripterine in simulated intestinal fluid was more than 80% at 6 h. Conclusion The formulation and preparation process are practical and simple, and these beads have great potentialities for carrying hydrophobic drug.