新型W/O/O法BSA/PLGA微球的制备、表征及体外细胞活性的研究  

Preparation and Characterization of BSA/PLGA Microspheres with a Novel W/O/O Method and Cell Viability in Vitro

作　　者：冯佳 张晓云[1] 尚青[1] FENG Jia, ZHANG Xiaoyun, SHANG Qing(College of Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Hebei Shijiazhuang 050018,Chin)

机构地区：[1]河北科技大学化学与制药工程学院,河北石家庄050018

出　　处：《河北师范大学学报（自然科学版）》2018年第2期138-147,共10页Journal of Hebei Normal University：Natural Science

基　　金：河北省自然科学基金(C2011208111)

摘　　要：选用牛血清白蛋白(BSA)为模型药物,聚乳酸-聚乙羟基醇共聚物(PLGA)为药物载体,通过水/油/油(W/O/O)新型凝聚法进行BSA/PLGA缓释微球的制备,考察PLGA的浓度、分子量、二氯甲烷(DCM)和硅油体积比、搅拌转速、固化溶剂及干燥方式等各个因素对制备过程的影响,并对其形貌、粒径、载药量和包封率等进行分析与表征,从而确定最佳的BSA/PLGA缓释微球的制备处方和工艺.结果表明:微球圆整均匀、平均粒度是75μm,包封率达85%;红外扫描图显示PLGA和BSA分子之间形成新的氢键,BSA被包裹在PLGA微球中;DSC图谱显示BSA被包裹在其中呈无定型状态;体外细胞活性实验中,3T3的细胞活性在80%以上,具有安全性.通过W/O/O新型凝聚法制备BSA/PLGA缓释微球的工艺较为稳定,包封率较高,载药量为4.58%.By using BSA as a protein model drug and,poly lactic acid-poly hydroxy alcohol copolymer（PLGA）as drug carrier,the PLGA microspheres were fabricated with a W/O/O coagulation method.The influence factors（i.e.PLGA concentrations,molecular weights,DCM/dimethylsilane ratios,stirring rates,curing solvent and drying method etc.）on microspheres morphology were studied.Through the analysis and characterization of morphology,particle size,drug loading and encapsulation efficiency,the best prescription for BSA/PLGA sustained-release microspheres and preparation process was obtained.The results show that the microspheres are round with the average particle size of 75μm,and the encapsulation efficiency is 85%.The new hydrogen bond between PLGA and BSA molecule in FTIR spectrais confirmed for the fabrication of BSA/PLGA microspheres.The DSC curves indicate that BSA are loaded in the surface and inner of PLGA microspheres,which is beneficial to improve the release profiles of BSA.Results showed that the BSA/PLGA microspheres had spherical shape and smooth surface without pores.In vitro cell viability,the cell activity concentration of 3 T3 was above 80% and was safe.BSA/PLGA sustained releasemicrospheres could be prepared by W/O/O coacervation,the process was stable,the encapsulation efficiency was 85%,and the drug loading rate was 4.58%.

关 键 词：牛血清白蛋白 PLGA微球 W/O/O法 制备工艺 分析与表征 

分 类 号：R945[医药卫生—微生物与生化药学]