天然产物研究与开发 ›› 2016, Vol. 28 ›› Issue (5): 724-727.doi: 10.16333/j.1001-6880.2016.5.015

• 研究简报 • 上一篇    下一篇

载10-甲氧基喜树碱缓释纳米粒的制备、表征与体外释药研究

李思阳1,孔庆新1,张瑞2,王洋2*   

  1. 1 江苏食品药品职业技术学院,淮安223003;2 东北林业大学盐碱地生物资源环境研究中心 东北油田盐碱植被恢复与重建教育部重点实验室,哈尔滨150040
  • 出版日期:2016-05-28 发布日期:2016-09-06

Preparation,Characterization and in vitro Release Behavior of 10-Methoxycamptothecin loaded Sustained Release Nanoparticles

LI Si-yang1,KONG Qing-xin1,ZHANG Rui1,WANG Yang2*   

  1. 1 Jiangsu Food & Pharmaceutical Science College,Huaian 223003,China; 2 Alkali Soil Natural Environmental Science Center,Northeast Forestry University,Key Laboratory of Saline alkali Vegetation Ecology Restoration in Oil Field,Ministry of Education,Harbin 150040,China
  • Online:2016-05-28 Published:2016-09-06

摘要: 以高分子多聚物聚乳酸(PLA)为材料,10-甲氧基喜树碱(MeOCPT)为模型药物,采用乳化溶剂挥发法制备载10-甲氧基喜树碱缓释纳米粒,表征并考察其体外释药特性。透射电子显微镜观察缓释纳米粒具有明显的球状结构,确定了最佳投料比为0.02:1,平均粒径在100~250 nm之间,包封率和载药量分别为83.57±3.45%和3.10±1.19%,体外持续缓慢释放达48 h以上,累计释放率超过70%,缓释效果明显。以乳化溶剂挥发法成功制备的载10-甲氧基喜树碱缓释纳米粒,为聚乳酸作为药物缓控释载体的进一步研究提供依据,为难溶性小分子药物研究提供方向。

关键词: 10-甲氧基喜树碱, 纳米粒, 制备, 表征, 体外释放

Abstract: The polylactic acid(PLA) was used as the material with 10-methoxycamptothecin(MeOCPT) as model drugs,the sustained-release nanoparticles for MeOCPT was successfully prepared and characterized by emulsion solvent evaporation method.The sustained-release nanoparticles was obvious spherical structure by transmission electron microscopy(TEM) observations.The optimal ratio of MeOCPT to PLA was 0.02:1.The particle size distribution was 100250 nm.The satisfactory encapsulation efficiency and drug-loading content were up to 83.57±3.45 and 3.10±1.19%,respectively.The in vitro release studies showed that 70% of MeOCPT was released from the sustained-release nanoparticles in the first 48 h which had obvious slow release effect.In conclusion,the sustained-release nanoparticles for MeOCPT were successfully prepared by emulsion solvent evaporation method which providing basis for further research of PLA as drug controlled release carrier and direction for the research of small molecular drugs.

Key words: 10-methoxycamptothecin, nanoparticles, preparation, haracterization, in vitro release

中图分类号: 

R283.6