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目的:考察多糖颗粒复合PLGA微球用作脉冲式释药系统的可行性。方法:用水相-水相乳化法将模型蛋白BSA包裹于多糖颗粒中,再用S/O/W法制备多糖颗粒复合PLGA微球。采用microBCA法测定该微球体外释放行为,并与W/O/W复乳法制备的BSA微球相对照。结果:用W/O/W复乳法制备的BSA微球的体外释放曲线显示,该微球在开始释放第一天起就出现一个平台期,之后则产生一个持续高释放量的行为。而多糖颗粒复合PLGA微球的体外释放曲线显示,其在释放第一天和一个较长平台期之后都出现峰形释放,相对于前者微球与脉冲释药模式更为相近。平台期时长与高分子性质有关,PLGA结构中乳酸相对于乙醇酸比例越高则平台期越长。结论:多糖颗粒复合PLGA微球具有良好的脉冲式释药效果,是一种较有前景的脉冲释药系统。
OBJECTIVE: To investigate the feasibility of using polysaccharide-loaded PLGA microspheres as a pulsatile drug delivery system. Methods: The model protein BSA was encapsulated in polysaccharide particles by water phase and aqueous phase emulsification, and the polysaccharide particles were prepared by S / O / W method. The in vitro release behavior of the microspheres was determined by microBCA method and compared with BSA microspheres prepared by W / O / W double emulsion method. Results: The in vitro release curves of BSA microspheres prepared by W / O / W double emulsion showed that the microspheres appeared a plateau on the first day after release, followed by a sustained high release. The in vitro release curves of the polysaccharide-loaded PLGA microspheres showed that the release peak appeared on the first day and after a long plateau phase, which was more similar to the former model. The duration of the platform is related to the nature of the polymer. The higher the proportion of lactic acid to glycolic acid in PLGA structure, the longer the plateau. CONCLUSION: The PLGA microspheres with polysaccharide particles have a good pulsatile release effect and are a promising pulsatile drug delivery system.