【摘要】 目的　制备bFGF PLGA微球 ,考察其一般性质、体外释药特性和微球中bFGF生物活性保存情况。方法　应用复乳干燥法制备缓释bFGF PLGA微球 (bFGF PLGA Ms) ,并考察其一般性质。采用ELISA法建立用于bFGF含量测定的标准方法和回归方程 ,模拟体内条件研究微球体外释药特性。将bFGF PLGA Ms加入成纤维细胞培养液中 ,MTT法观察细胞增殖情况。结果　微球表面光滑圆整 ,球体均匀度好 ,平均粒径为 (1 5 5 2± 0 0 15 ) μm ,冻干粉剂为白色粉末状 ,再分散性良好 ,临界相对湿度为6 4 % ,CH2 Cl2 残留量低于限量的 1/10 ,微球包封率和载药量分别为 (6 6 4 3± 1 2 4 ) %和 [(2 7 18± 0 5 1)× 10 -3 ]%。微球体外释药规律符合Higuichi方程 :Q =2 5 884 6t1/ 2 - 15 70 5 1(r =0 9975 ) ,突释期内释放度仅为 19 2 6 % ,11d后其释放度达到72 4 7%。培养初期 ,bFGF组A值高于其余两组 ;培养中后期 ,PLGA微球组A值高于其余两组 ,差异均有显著性意义 (q检验 ,P <0 0 5 )。结论　bFGF PLGA微球及其冻干粉剂制备工艺良好 ;微球中bFGF生物活性保存良好 ,体外具有明显缓释作用。更多还原

【Abstract】 OBJECTIVE To prepare bFGF-PLGA microspheres (bFGF-PLGA -Ms) and investigate their general properties, in vitro drug release characteristics and biologic activity of bFGF released from the microspheres. METHODS The bFGF-PLGA microspheres were prepared by w/o/w multiple emulsion volatilizing method. Their general properties were observed. To measure the content of bFGF, ELISA method was used and the regression equation was established. The bFGF-PLGA -Ms were kept in 0.9% sodium chloride solution to study their in vitro release characteristics. The proliferation of the cultured fibroblast was measured with MTT method after bFGF-PLGA -Ms being added to the DMEM culture medium. RESULTS The bFGF-PLGA-Ms were good, even and uniform spheres with mean particle size of (1.552±0.015)μm. The lyophilized powder was pure white with good dispority. Its critical humidity was 64%. The content of CH 2Cl 2 was less than 1/10 of the limited value. The drug loading amount and encapsulation efficiency of bFGF-PLGA-Ms were [(27.18±0.51)×10 -3 ]% and (66.43±1.24)% respectively. The in vitro release profile of bFGF-PLGA -Ms was figured by Higuichi equation: Q =25.884?6 t 1/2 -15.705?1 ( r =0.997?5). The drug release rate was only 19.26% during the burst release phase and rose to 72.47% at the 11th day. 2 and 3 days after plate culturing, the absorption values at 490 nm of bFGF group were much higher than those of the bFGF-PLGA-Ms group and the PLGA group; 4 to 6 days after plate culturing, the A values of bFGF-PLGA -Ms group was the highest among the three groups. CONCLUSION The bFGF-PLGA-Ms and their lyophilized powder have excellent pharmaceutical properties showing sustained release effect in vitro with good biological activity.更多还原