程骥, 朱家壁, 杨泗兴, 王长斌. 支链淀粉修饰双嘧达莫脂质体的制备及其在小鼠体内的组织分布J. 药学学报, 2006, 41(3): 277-281.
引用本文: 程骥, 朱家壁, 杨泗兴, 王长斌. 支链淀粉修饰双嘧达莫脂质体的制备及其在小鼠体内的组织分布J. 药学学报, 2006, 41(3): 277-281.
CHENG Ji, ZHU Jia-bi, YANG Si-xing, WANG Chang-bin. Preparation of amylopectin modified dipyridamole liposome and its tissue distribution in miceJ. Acta Pharmaceutica Sinica, 2006, 41(3): 277-281.
Citation: CHENG Ji, ZHU Jia-bi, YANG Si-xing, WANG Chang-bin. Preparation of amylopectin modified dipyridamole liposome and its tissue distribution in miceJ. Acta Pharmaceutica Sinica, 2006, 41(3): 277-281.

支链淀粉修饰双嘧达莫脂质体的制备及其在小鼠体内的组织分布

Preparation of amylopectin modified dipyridamole liposome and its tissue distribution in mice

  • 摘要: 目的研究支链淀粉修饰双嘧达莫(DIP)脂质体的制备方法并考察其在小鼠体内的组织分布。方法 采用薄膜-分散法制备普通DIP脂质体;合成两亲性的棕榈酰化支链淀粉并用其修饰DIP脂质体;比较修饰前后包封率、zeta电位、平均粒径和径距的变化;采用反相高效液相法测定小鼠组织中的DIP浓度。结果修饰后DIP脂质体的包封率降低,zeta电位增加,平均粒径和径距无明显变化;普通脂质体可以增强DIP在肺部、肝脏和脾脏的分布,而较之普通脂质体,支链淀粉修饰的脂质体可以进一步增加肺部DIP水平,同时减少DIP在肝脏和脾脏的分布,并延长在肺部的滞留时间。结论与普通脂质体和注射液比较,支链淀粉修饰的脂质体可以改变DIP在小鼠体内的组织分布,具有显著的肺靶向性。

     

    Abstract: AimTo prepare amylopectin anchored dipyridamole (DIP) liposome and to study its tissue distribution in mice. MethodsThe regular DIP liposomes were prepared by film-scatter method. The amphiphilic O-palmitoyl amylopectin was synthesized and added to modify the surface of liposome. The entrapping efficiency, zeta potential, mean diameter, span of modified and regular liposomes were assayed. The RP-HPLC was used for the determination of DIP concentration in mice tissue. Results After modification, the entrapping efficiency depressed, zeta potential was raised, mean diameter and span had no obvious change. The level of DIP in lung, liver and spleen for regular liposomes were higher than that of injections. Compared with regular liposomes, the modified liposomes increased the DIP level in lung, and decreased the DIP level in liver, spleen, moreover, lengthened the retention time of DIP in lung. ConclusionThe distribution of modified liposome in mice was markedly changed as compared with regular liposomes and injections. The modified liposomes had obvious lung targeting property.

     

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