复方总黄酮聚乳酸-羟基乙酸共聚物微囊的制备及体外释药特性  

Preparation of compound TF-PLGA microcapsule and its drug release characteristics in vitro

作　　者：陈楠楠[1] 马宁[1] 车鸿泽 焦鹏[1] 陈飞[1] 张莉[2] CHEN Nannan MA Ning CHE Hongze JIAO Peng CHEN Fei ZHANG Li(Department of Periodonties, Stomatology Hospital, JilinUniversity, Changchun 130021, China Departmentof Emergency, Stomatology Hospital, Jilin University, Changchun130021, China)

机构地区：[1]吉林大学口腔医院牙周病科,吉林长春130021 [2]吉林大学口腔医院急诊科,吉林长春130021

出　　处：《吉林大学学报（医学版）》2017年第3期593-599,I0004,共8页Journal of Jilin University：Medicine Edition

基　　金：吉林省中医药管理局科研项目资助课题(2014-Q48)

摘　　要：目的:以聚乳酸-羟基乙酸共聚物(PLGA)作为载体材料制备复合骨碎补总黄酮(TFRD)和野菊花总黄酮(TFC)的TF-PLGA缓释微囊,探讨微囊的最佳制备工艺及其体外缓释特性。方法:以PLGA、TFRD和TFC为原料,采用复乳-溶剂挥发法制备TF-PLGA缓释微囊;以包封产率(EE)为评价指标,通过单因素实验及正交实验进行工艺优化,筛选最佳的工艺参数;光学显微镜(LM)和扫描电子显微镜(SEM)下观察微囊的形态特征、粒径大小和分布情况;采用提取法测定TF-PLGA微囊的体外累计释药率并绘制累计释放曲线。结果:单因素实验和正交实验优化的最佳制备工艺,PLGA浓度为140g·L^(-1),油相体积为1.4mL,乳化速度为1 500r·min^(-1),乳化时间为5min。优化后微囊平均EE为(83.89±2.30)%,平均实际载药量(DL)为(5.90±0.07)%;LM和SEM下观察,微囊形态圆整,平均粒径为(44.34±14.68)μm,粒径分布较窄;体外释放实验检测,24h累计释药率达40%,第50天后累积释药率超过90%。结论:TF-PLGA缓释微囊具有优良的载药及缓释效果,制备工艺简单,重复性良好。Objective：To use polylactic-co-glycolic acid（PLGA） as vector material to prepare the compound total flavonoids of Rhizoma Drynariae（TFRD） and total flavonoids of Chrysanthemum（TFC） sustained release microcapsule TF-PLGA microcapsules,and to investigate the the best preparation technique of TF-PLGA microcapsules and their sustained release characteristics in vitro.Methods：The TF-PLGA microcapsules were prepared with TFRD,TFC,and PLGA by emulsifying-solvent evaporation technique under certain conditions.With the encapsulation efficiency（EE） as the evaluation indicator,the optimal formulation was verified by single factor experiment and orthogonal design;the general morphology,the particle size and distribution of the microcapsules were observed by light microscope（LM） and scanning electron microscope（SEM）;the cumulative drug release rate of TF-PLGA microcapsules was detected by constant temperature commotion method in vitro and the release curves of the TF-PLGA were drawn.Results：The optimal prescription was as follows：the concentration of PLGA was 140 g·L^-1,oil phase volume was 1.4 mL,emulsifying speed was 900 r·min-1,emulsifying time was 5 min,the average EE was（83.89±2.30）%,and the average drug loading rate（DL） was（5.90±0.07）%.The LM and SEM resluts showed that the TF-PLGA microcapsules presented as round ball,the average particle size was（44.34±14.68）μm,and the distribution was relatively narrow.The drug release in vitro results showed that the initial drug release rate（24 h）was about 40%,and the cumulative drug release rate was over 90% after 50 d.Conclusion：The TF-PLGA sustained release microcapslue has better drug-loaded and sustained-release effects with simple preparation technique and better repeatability.

关 键 词：骨碎补总黄酮 野菊花总黄酮 聚乳酸-羟基乙酸 微囊 缓释 

分 类 号：R781.4[医药卫生—口腔医学]