化学学报 ›› 2011, Vol. 69 ›› Issue (05): 508-514. 上一篇    下一篇

研究论文

高包封率异烟肼类脂质体的制备与性质研究

杨占娴, 宫永宽   

  1. (合成与天然功能分子化学教育部重点实验室 西北大学化学与材料科学学院 西安 710069)
  • 收稿日期:2010-07-18 修回日期:2010-11-11 出版日期:2011-03-14 发布日期:2010-11-25
  • 通讯作者: 宫永宽 E-mail:gongyk@nwu.edu.cn
  • 基金资助:

    国家自然科学基金项目

Preparation and Property of Liposome with Isonicotinyl Hydrazide Phospholipid Derivative for High Encapsulation Efficiency

YANG Zhan-Xian, GONG Yong-Kuan   

  1. (Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, College of Chemistry & Materials Science, Northwest University, Xi an 710069)
  • Received:2010-07-18 Revised:2010-11-11 Online:2011-03-14 Published:2010-11-25

以异烟肼为模型药物, 合成了异烟肼取代卵磷脂疏水链的两亲性异烟肼磷脂衍生物. 用薄膜超声分散法将其制备成脂质体, 从而将异烟肼脂质体的药脂比从0.1~0.3提高至2.0, 包封率由2%提高到接近100%. 通过调节超声处理时间和磷脂浓度可制得粒径大小可控的脂质体. 体外释药研究表明, 该脂质体具有明显的控制释放性能. 这种以药物分子取代卵磷脂疏水链的两亲性磷脂衍生物制备脂质体的方法, 为难包封于脂质体的药物实现高包封率提供了新途径.

关键词: 脂质体, 包封率, 异烟肼, 磷脂衍生物, 药物控释

Isonicotinyl hydrazide (INH) was chosen as a model drug, and was covalently attached to glyceryl phosphatide as the hydrophobic moieties of the phospholipid derivative. Isonicotinyl hydrazide phospholipid derivative liposome was prepared by thin-film hydration and sonication method. Drug encapsulation efficiency and drug to lipid molar ratio of the liposome were increased from 2% to nearly 100% and from 0.1~0.3 to 2.0 respectively. Liposomes with different sizes were prepared by controlling concentration of the phospholipid derivative and sonication time. The liposomes showed remarkable controlled drug release property when compared with a free drug. This novel liposome provides a new way for encapsulating drugs more especially.

Key words: liposome, encapsulation efficiency, isoniazid, phospholipid derivative, controlled release

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