吉林大学学报(医学版) ›› 2017, Vol. 43 ›› Issue (03): 593-599.doi: 10.13481/j.1671-587x.20170325

• 基础研究 • 上一篇    下一篇

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

陈楠楠1, 马宁1, 车鸿泽1, 焦鹏1, 陈飞1, 张莉2   

  1. 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
  • 收稿日期:2017-01-05 出版日期:2017-05-28 发布日期:2017-06-01
  • 通讯作者: 张莉,副教授,硕士研究生导师(Tel:0431-85579359,E-mail:zlamy1009@sina.com) E-mail:zlamy1009@sina.com
  • 作者简介:陈楠楠(1990-),女,吉林省公主岭市人,在读医学硕士,主要从事牙周病学方面的研究。
  • 基金资助:
    吉林省中医药管理局科研项目资助课题(2014-Q48)

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

CHEN Nannan1, MA Ning1, CHE Hongze1, JIAO Peng1, CHEN Fei1, ZHANG Li2   

  1. 1. Department of Periodontics, Stomatology Hospital, JilinUniversity, Changchun 130021, China;
    2. Departmentof Emergency, Stomatology Hospital, Jilin University, Changchun 130021, China
  • Received:2017-01-05 Online:2017-05-28 Published:2017-06-01

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140 g·L-1,油相体积为1.4 mL,乳化速度为1500 r·min-1,乳化时间为5 min。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。

关键词: 骨碎补总黄酮, 微囊, 野菊花总黄酮, 聚乳酸-羟基乙酸, 缓释

Abstract: 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 microcapsuleTF-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.

Key words: total flavonoids of Rhizoma Drynariae, total flavonoids of Chrysanthemum, slow-release, polylactic-co-glycolic acid, microcapsules

中图分类号: 

  • R781.4