骨形成白微球温敏性凝胶复合系统的制备及释药特性研究.docVIP

骨形成蛋白微球温敏性凝胶复合系统的制备及释药特性研究 符旭东，刘宏，汤韧，张孟佑（广州军区武汉总医院药剂科，武汉，430070） 摘要 目的 考察了处方和制备工艺对人重组骨形成蛋白－2（BMP-2）（PLGA）BMP-2载药微球。以单甲基聚乙二醇－羟基乙酸共聚物（MPEG-PLGA）BMP-2微球，其突释明显小于以PLGA为材料制备的微球，增加内水相与油相的体积比、在内水相中加入氯化钠均可以在一定程度上减小突释。结论 BMP微球温敏性凝胶复合系统制备工艺，具有比rhBMP-2微球剂更理想的体外释药特性。 关键词：人重组骨形成蛋白－2; 聚乳酸-乙醇酸共聚物；单甲基聚乙二醇－羟基乙酸共聚物; 微球；温敏性凝胶；突释 Preparation of recombinant human bone morphogenetic protein-2 Loaded microspheres/ thermosensitive hydrogels complex and its in vitro release characteristic Fu Xu-dong , Liu Hong，Tang Ren, Zhang Meng-you（Wuhan General Hospital of Guanzhou Command, Wuhan 430030） ABSTRACT To examine the effects of formulation factors on in vitro release rate of recombinant human bone morphogenetic protein-2 (rhBMP-2) loaded microspheres and compare drug release profiles of microspheres and microspheres/ thermosensitive hydrogels complex. METHODS Blank microspheres were prepared with W/O/W emulsion solvent evaporation method.RhBMP-2 loaded microspheres was prepared with absorption method. Thermosensitive hydrogels were prepared with MPEG-PLGA.Enzyme-linked immunosorbent assay was used to determine drug content and in vitro release rate. RESULTS The profiles of RhBMP-2 microspheres were characterized by three phase, while the in vitro release profile of rhBMP-2 microspheres/ thermosensitive hydrogels complex conformed to Higuchi equation. The amount of rhBMP-2 released from microspheres in the initial burst phase was decresed markedly when PLGA-COOH was used to prepare microspheres instead of PLGA. Increasing the volume ratio of internal aqueous and adding NaCL to internal aqueous phase could reduce initial release. CONCLUSION Rhbmp2 –loaded microspheres/ thermosensitive hydrogels complex exerted a desirable release characteristic. KEY WORDS recombinant human bone morphogenetic protein-2; PLGA; MPEG-PLGA; thermosensitive hydrogels; microsphere；initial burst release 牙周病是世界卫生组织列为重点防治的、人类普遍罹患的口腔疾病之一，是成年人失牙的主要原因最终目标是实现牙周组织包括牙槽骨、牙骨质和牙周膜的完全功能性再生，而牙周组织再生的基础是牙周膜细胞（PDLCs），但在牙周损伤部位PDLCs