PLGA微球用于蛋白/多肽类药物缓释递送的优化策略  

Optimization Strategy of PLGA Microspheres for Sustained-release Delivery of Protein/Polypeptide Drugs

作　　者：郭作娟 梁荣财[1,2] GUO Zuojuan;LIANG Rongcai(Key Lab.of Molecular Pharmacology and Drug Evaluation,Ministry of Education,Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong,School of Pharmacy,Yantai University,Yantai 264005;State Key Lab.of Long-Acting and Targeting Drug Delivery System,Shandong Luye Pharmaceutical Co.,Ltd.,Yantai 264003)

机构地区：[1]烟台大学药学院,新型制剂与生物技术药物研究山东省高校协同创新中心,分子药理和药物评价教育部重点实验室(烟台大学),山东烟台264005 [2]山东绿叶制药有限公司,长效和靶向制剂国家重点实验室,山东烟台264003

出　　处：《中国医药工业杂志》2023年第3期312-319,共8页Chinese Journal of Pharmaceuticals

摘　　要：传统的蛋白/多肽类药物微球存在突释、迟滞释放和不完全释放等缺陷,而利用可生物降解的聚丙交酯-乙交酯(PLGA)微球递送蛋白/多肽类药物能实现缓释给药,提高患者依从性。该文首先分析了影响微球释药性能的各种因素,然后从载体材料和制备工艺方面总结了多种改进策略,特别是对乳化溶剂挥发法中内水相的改造方法。此外,还介绍了微流控、超临界流体和自愈包封等新制备技术的应用,以及核壳结构微球控释系统的发展,以期为蛋白/多肽类药物微球的制备提供新思路。Traditional microspheres loaded with protein/polypeptide drugs have some shortcomings,such as burst release,delayed release,and incomplete release of protein/peptide drugs.However,microspheres with poly(lactide-co-glycolide)(PLGA)as carriers can achieve sustained release delivery of protein/polypeptide drugs and improve patient compliance.This paper analyzes the various factors that affect drug release performance of microspheres,and summarizes a variety of improvement strategies from the aspects of carrier materials and preparation technology,especially the remolding methods on the internal water phase in the emulsion-solvent evaporation method.Besides,the application of new technology,such as microfluidic,supercritical fluid,self-healing encapsulation,and the development of core-shell microspheres controlled-release drug delivery systems are also introduced to provide new ideas for the preparation of protein/polypeptide microspheres.

关 键 词：微球 PLGA 蛋白 多肽 核壳结构 

分 类 号：R944.9[医药卫生—药剂学]