中文摘要：

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．

英文摘要：

Isonicotinyl hydrazide （INH） was chosen as a model drug, and was covalently attached to glyc eryl phosphatide as the hydrophobic moieties of the phospholipid derivative. INH phospholipid derivative liposome was prepared by thin-film hydration and sonication method. The 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 the concentration of the phospholipid derivative and the time of sonication. Compared with the free drug, remarkable controlled drug release property was observed in the system of 1NH phospholipid derivative liposome. This novel liposome provides a new route for encapsulating drugs more efficiently.