载辛伐他汀PLGA缓释微球的制备及表征  

Preparation and Characterization of Simvastatin-loaded PLGA Microspheres for Sustained Release

作　　者：李祥伟[1] 王丽芹[1] 张颖丽[1] 刘金钟[2] 倪世磊[2] 史册[2] 孙宏晨[2] 

机构地区：[1]吉林大学口腔医院牙体牙髓科,吉林长春130021 [2]吉林大学口腔医院病理科

出　　处：《口腔医学研究》2013年第3期217-220,223,共5页Journal of Oral Science Research

基　　金：中央高校基本科研业务费项目;吉林省科技发展计划资助项目(编号:201101051)

摘　　要：目的:制备可生物降解并能促进牙槽骨形成的载辛伐他汀PLGA缓释微球。方法:通过乳化-溶剂挥发法制备PLGA微球及载辛伐他汀PLGA缓释微球,表征其形态、粒径,并计算载药量和包封率;用磷酸盐缓冲液(pH7.4)分散载药微球后置37℃水浴内,分别于1、3、5、7、14、28、56d检测上清液在238nm处的吸光度值,通过标准曲线方程计算辛伐他汀的浓度,计算累积释放量,绘制各组载药微球中辛伐他汀的释放曲线。结果:PLGA微球表面光滑、圆整,粒径范围358～1768nm。粒径随PLGA分子量的增加而递减;载辛伐他汀PLGA微球表面光滑、圆整,无粘连,粒径范围213～8430nm,微球表面可见微孔,载药量为0.99%～10.17%,包封率为10.97%～40.67%。随着载药微球的降解,辛伐他汀缓释速率较平缓,释放时间达8周以上。结论:乳化-溶剂挥发法可制备形态规整且分散良好的载辛伐他汀PLGA缓释微球,载药微球可通过生物降解缓释辛伐他汀,释药时间达8周以上。Objective： To prepare biodegradable simvastatin-loaded PLGA microspheres（SLPM） that are able to release simvastatin slowly and promote alveolar bone formation. Methods： SLPM and blank PLGA microspheres were prepared by emulsion-solvent evaporation method respectively. The diameter, surface morphology, drug loading and entrapment efficiency of the microspheres were measured and calculated. The SLPM was dispersed in PBS（pH7.4） and bathed at 37℃. After that, the supernatant was gained and measured by UV at 238 nm to calculate the concentration of simvastatin through a standard curve equation at 1,3,5,7,14,28,56 days respectively. And then, the cumulation release curve of simvastatin was drawn. Results： Both SLPM and blank PLGA microspheres are round, regular and well dispersed. Its diameter decreases with PLGA molecular weight increasing. The diameter range of blank PLGA microspheres and SLPM are 358--1768nm and 213-8430nm respectively. Some micro-holes can be seen on the surface Of SLPM. The drug loading is 0. 99-10.17% and entrapment efficiency is 10.97% -40.67%. The SLPMs degrade continuously and keep on releasing simvastatin for over 8 weeks. Conclusion： Emulsion-solvent evaporation method is an ideal way to prepare SLPM. Simvastatin could be released slowly from biodegradebale SLPM for over 8 weeks.

关 键 词：PLGA 辛伐他汀 缓释 微球 

分 类 号：R782[医药卫生—口腔医学]