吡喹酮聚乳酸乙醇酸微球的制备和表征

摘要

采用O/W溶剂挥发法,以聚乳酸乙醇酸(PLGA)为基质材料制备了吡喹酮(PZQ)微球,并用HPLC、SEM、XRD和FTIR对药物进行了含量测定、形态观测,以及对药物在微球中的物理状态和药物与材料间是否存在相互间的作用力进行考察.结果表明:PZQ微球的包封率高达94.8%,微球外观圆整,表面多孔,结晶型的PZQ以无定型或分子状态分散于微球中,药物与聚合物材料PLGA没有相互间的作用力.载药微球包封率高,改变工艺条件对微球包封率影响很小,说明PLGA是一种合适包裹PZQ的载体材料.%This paper aimedto prepare and characterize PZQ loaded PLGA microspheres.The PLGA microspheres were prepared by O/Wemulsion-solvent evaporation method.The drug content,drug release in vitro,the morphology of the microspheres,the physical state of the drug in the microspheres and the interaction between drugs and materials were determined respectivelyby HPLC,SEM, XRD and FTIR.The encapsulation efficiency of microspheres wasas high as 94.8%,the morphology of microspheres wereround and the surface of microspheres were porous.The crystalline PZQformed as amorphous or molecular state in the microspheres.There was no molecular interaction between PZQ and PCL, whichcould solve the problem of first pass effect and fast metabolism in vitro.The encapsulation efficiency of drug loaded microspheres was high and the influence of process conditions on the encapsulation efficiency was very small,which indicated that PLGA was a suitable carrier material for PZQ.