高等学校化学学报 ›› 2010, Vol. 31 ›› Issue (11): 2298-2302.

• 研究论文 • 上一篇    下一篇

可生物降解固体脂质纳米粒的制备、表征及药物的体外释放

管清香1, 朱昆2, 林天慕1, 管庆涛2, 郭杰3, 尹建元1   

  1. 1. 吉林大学药学院, 长春 130021;
    2. 吉林大学中日联谊医院, 长春 130033;
    3. 吉林大学公共卫生学院, 长春 130021
  • 收稿日期:2010-01-18 出版日期:2010-11-10 发布日期:2010-11-10
  • 通讯作者: 尹建元. E-mail: yinjy@jlu.edu.cn; 郭杰. E-mail: guojie@jlu.edu.cn
  • 基金资助:

    吉林省中医药管理局资金(批准号: 2006zy19)资助.

Preparation, Characterization and Drug Release of Biodegradable Solid Lipid Nanoparticles

GUAN Qing-Xiang1, ZHU Kun2, LIN Tian-Mu1, GUAN Qing-Tao2, GUO Jie3*, YIN Jian-Yuan1*   

  1. 1. School of Pharmacy, Jilin University, Changchun 130021, China;
    2. China-Japan Union Hospital, Jilin University, Changchun 130033, China;
    3. School of Public Health, Jilin University, Changchun 130021 China
  • Received:2010-01-18 Online:2010-11-10 Published:2010-11-10
  • Contact: YIN Jian-Yuan. E-mail: yinjy@jlu.edu.cn; GUO Jie. E-mail: guojie@jlu.edu.cn
  • Supported by:

    吉林省中医药管理局资金(批准号: 2006zy19)资助.

摘要: 以可生物降解材料硬脂酸为载体, 以葛根总黄酮为模型药物, 采用乳化蒸发-低温固化法制备固体脂质纳米粒. 采用透射电镜研究载药纳米粒形态, 激光粒度分析仪测定其粒径, X射线衍射仪进行物相鉴别, 并对纳米粒的包封率及体外释药特性等进行了研究. 分析结果表明, 所制备硬脂酸固态脂质纳米粒为类球实体, 粒径分布比较均匀, 平均粒径为(263.82±3.6) nm, 包封率为(67.53±0.12)%. X射线衍射分析证明药物以分子或细小粒子分散于脂质骨架中. 体外释药研究结果表明, 纳米粒体外释药先快后慢, 12 h累积释药50%, 包封于降解材料骨架内的药物通过骨架溶蚀缓慢释放. 药物的体外释放符合Higuchi方程.

关键词: 生物降解, 硬脂酸, 固态脂质纳米粒, 葛根总黄酮, 物相分析

Abstract: Biodegradable solid lipid nanoparticles loaded with pueraria flavones(PF-SLN) were prepared by emulsification evaporation-solidification at low temperature with a biodegradable material, stearic acid as the carrier. The morphology and particle size of PF-SLN were measured by TEM and laser light scattering technique, respectively. The physical status of the drug in PF-SLN was analyzed by X-ray powder diffractometry. Its entrapment efficacy in SLN and release were also investigated. PF-SLN is near spherical in shape and the average diameter is (263.82±3.6) nm. Its entrapment effciency (EE) is (67.53±0.12)%. X-ray powder diffraction analysis results show that the pueraria flavones are dispersed with the state of molecular or tiny particles in the matrix of SLN. The results show that the release of PF-SLN occurs rapidly in the early stage and then slowly which accumulate up to 50% in 12 h . The drug release slowly from SLN following matrix erosion. The release profile fits well to the Higuchi equation.

Key words: Biodegradable, Stearic acid, Solid lipid nanoparticle, Pueraria flavone, Material phase analysis