负载川芎嗪-PLGA微球的制备及体外缓释性能研究

Study on the preparation and in vitro release characterization of tetramethylpyrazine–PLGA sustained release microspheres

目的运用复乳-溶剂挥发法制备川芎嗪-PLGA微球,并测定载药微球的理化性质,绘制体外释药曲线。方法选用传统O/W型乳化-溶剂挥发法制备川芎嗪-PLGA微球,光镜及扫描电镜下观察形态形状,公式计算包封率及载药量。溶解后,分光光度法定时测定释放的药物浓度,绘制载药微球的体外释放曲线。结果光学显微镜及扫描电镜下观察,川芎嗪-PLGA微球成球规整,表面光滑,分布较均匀,成球形态饱满,微球包封率(79.4±3.31)%,载药量(7.8±0.24)%,体外释放突释率为(19.57±2.14)%,28 d累积释放药量达(74.82±0.92)%。结论PLGA微球是川芎嗪较为理想的缓释载体,包封率及载药量适宜,体外释放具有良好的缓释性,突释效应小。缓释微球能够延长所载川芎嗪的作用时间,减少给药次数,从而增强患者的适应性。

Objective To study the preparation of Ligustrazine PLGA microspheres by double emulsion solvent evaporation method,and determine the physicochemical properties of the microspheres,and draw the drug release curve in vitro.Methods Ligustrazine PLGA microspheres were prepared by traditional O/W emulsion solvent evaporation method.The morphology and shape were observed under light microscope and scanning electron microscope.The encapsulation efficiency and drug loading were calculated by formula.After dissolution,the drug concentration was determined by spectrophotometry,and the in vitro release curve of drug loaded microspheres was drawn.Results under the light microscope and scanning electron microscope,the microspheres were regular in shape,smooth in surface,evenly distributed and full in shape.The encapsulation efficiency of the microspheres was(79.4±3.31)%,the drug loading was(7.8±0.24)%,the burst release rate in vitro was(19.57±2.14)%,and the cumulative release amount in 28 days was(74.82±0.92)%.Conclusion PLGA microsphere is an ideal sustained-release carrier for Ligustrazine with suitable entrapment efficiency and drug loading.The sustained-release microspheres can prolong the action time of Ligustrazine loaded,reduce the times of administration,and enhance the adaptability of patients.