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目的制备磷酸川芎嗪星型聚乳酸载药微球,研究制备工艺参数对载药微球的药物包封率的影响,并对其体外释放特性进行表征。方法以星型聚L-乳酸(sPLLA)为聚合物基材,采用复乳-溶剂挥发法制备磷酸川芎嗪(LP)星型聚乳酸载药微球(sPLLA/LP),采用正交试验优化处方,研究sPLLA/LP的体外缓释特性,并用FT-IR和SEM对微球进行表征。结果通过极差分析与方差分析建立sPLLA/LP的药物包封率与制备工艺参数之间的关系,并在此基础上遴选出优化工艺。LP与sPLLA结合良好,sPLLA/LP微球缓释7 d后,sPLLA出现部分降解。采用优化工艺所制备的sPLLA/LP微球具有良好的缓释效果,SEM分析与缓释模型的拟合结果表明,0~48h阶段的释药机制为药物扩散和聚合物降解协同作用;48~144 h阶段则主要为药物扩散释药。结论采用复乳-溶剂挥发法制备的sPLLA/LP微球的药物包封率较高、体外释药平稳。
OBJECTIVE To prepare tetramethylpyrazine phosphate-loaded poly (DL-lactide-co-glycolide) microspheres and investigate the effect of preparation parameters on drug entrapment efficiency of drug-loaded microspheres and to characterize its in vitro release characteristics. Methods The star polylactic acid-loaded microspheres (sPLLA / LP) were prepared by double-emulsion-solvent evaporation method using sPLLA as the polymer matrix. The orthogonal design Prescription, to study sPLLA / LP sustained-release characteristics in vitro and microspheres were characterized by FT-IR and SEM. Results The relationship between the entrapment efficiency of sPLLA / LP and preparation process parameters was established by range analysis and analysis of variance (ANOVA). Based on this, the optimization process was selected. LP and sPLLA combined well, sPLLA / LP microspheres after partial release of 7d, sPLLA partial degradation. The sPLLA / LP microspheres prepared by the optimized process had good sustained-release effect. The fitting results of the SEM analysis and the sustained-release model showed that the drug release mechanism during the 0-48h phase was the synergistic effect of drug diffusion and polymer degradation; In the 144 h stage, drug release was mainly released. Conclusion The encapsulation efficiency of sPLLA / LP microspheres prepared by double emulsion-solvent evaporation method is high and the drug release in vitro is stable.