肺靶向炎琥宁明胶微球的制备

Studies on Preparation of Lung-targeting Potassium Sodium Dehydroandroan Drographolide Succinate Gelatin Microspheres

目的对炎琥宁肺靶向明胶微球的处方、工艺、释药特性及其体内靶向性进行研究。方法以生物降解材料明胶为载体,采用乳化交联法制备炎琥宁明胶微球;单因素考察的基础上,利用正交实验设计筛选最佳处方和工艺;考察其体外释药特性;兔耳缘静脉注射微球后,取肺组织切片,体内试验结果初步考察其肺靶向性。结果所制备的炎琥宁明胶微球外形圆整,大小均匀,平均粒径为17.14μm,载药量为2.08%,包封率为70.94%;1.5 h体外释放50%左右,12 h可达90%以上。体内试验结果初步验证其具有一定肺靶向性。结论筛选的最佳处方工艺可制备性质优良的炎琥宁肺靶向明胶微球。

OBJECTIVE To prepare the potassium sodium dehydroandroan drographolide succinate gelatin microspheres （P-GMS）, study the releasing properties in vitro and the lung target characteristics in vivo. METHODS P-GMS were prepared by emulsion chemical cresslinking method using gelatin as wall material. Based on the result of slngle-factor selecting experiment, the formulations and the preparation methods were evaluated by orthogonal experiment method, The rabbit lung histological sections were observed by microscope after injecting the P-GMS to verify the lung target characteristics. RESULTS P-GMS were regular in morphology with a mean diameter of 17.14 μm. The drug loading amount was 2.08% and the encapsulation efficiency was 70.94%. The aceumulated releasing ratio in vitro was 50% at 1.5 h and reached 90% at 12 h. The initial experiment in vivo verified the lung target characteristics of the P-GMS. CONCLUSION P-GMS is a good lung-targeting drug release system.