利福平丝素蛋白载药微球的制备及性能研究

目的通过测定利福平丝素蛋白微球的载药量、包封率及释放度,考察乳化转速、有机溶剂与丝素蛋白溶液比例,对微球的制备方法进行优化,筛选微球的最佳制备方法。方法采用乳化法制备利福平丝素蛋白微球,以不同转速、有机溶剂与丝素蛋白溶液不同比例分别制备利福平丝素蛋白微球,采用扫描电镜观察微球的形态,用紫外分光光度法测定微球的载药量、包封率及释放度,以形态、载药量、包封率及释放度为指标,筛选微球的最佳制备方法。在此基础上,采用最佳处方制备3批利福平丝素蛋白微球,对微球的形态、粒径、包封率、载药量和释放度进行考察。结果有机溶剂与丝素蛋白溶液体积比为4∶1、转速为200 r·min^-1时所得利福平丝素微球形态均匀,近似球形,载药量和包封率较高,所得载药微球有较好的缓释作用。以最佳处方制得微球载药量为66.1%±0.87%,包封率为87.80%±2.23%。结论有机溶剂与丝素蛋白溶液体积比为4∶1、转速为200 r·min^-1时载药量、包封率和释放度较好,故选择此处方为利福平丝素蛋白微球的最佳制备处方。

Preparation and properties of rifampicin loaded microspheres

Objective By measuring the drug loading,encapsulation efficiency and release solution rate of rifampicin-like microspheres,the emulsification speed,organic solvent and silk fibroin solution ratio were investigated to optimize the preparation method of microspheres and to optimize the preparation of microspheres.Methods The rifampicin silk fibroin microspheres were prepared by emulsification method,and the rifampicin silk fibroin microspheres were prepared at different speeds,organic solvents and silk fibroin.The morphology of the microspheres was observe by scanning electron microscopy.The drug loading,encapsulation efficiency and release rate of the microspheres was by determine UV spectrophotometry.The optimal preparation conditions of microspheres were selected by morphology,drug loading,encapsulation efficiency and release rate.On this basis,3 batches of rifampicin-like protein microspheres were prepared and its morphology,particle size,encapsulation efficiency,drug loading and release of the microspheres were observed.Results The obtained rifampicin microspheres have uniform morphology,approximately spherical shape,particle size,high drug loading and encapsulation efficiency,under the conditions of volume ratio of organic solvent to silk fibroin solution 4∶1,rotation speed 200 r·min^-1.The drug loading is 66.1%±0.87%and the encapsulation efficiency is 87.80%±2.23%.Conclusion Microspheres have better drug loading rate,encapsulation efficiency and drug release rate under the 200 r·min^-1 and the volume ratio of organic solvent to silk fibroin 4∶1.