Cheng Ji, Zhu Jia-bi, Yang Si-xing, Wang Chang-bin
Pharmaceutical Research Institute, China Pharmaceutical University, Nanjing.
Yao Xue Xue Bao. 2006 Mar;41(3):277-81.
To prepare amylopectin anchored dipyridamole (DIP) liposome and to study its tissue distribution in mice.
The 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.
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.
The distribution of modified liposome in mice was markedly changed as compared with regular liposomes and injections. The modified liposomes had obvious lung targeting property.
制备支链淀粉锚定双嘧达莫（DIP）脂质体并研究其在小鼠体内的组织分布。
采用薄膜分散法制备常规DIP脂质体。合成两亲性O-棕榈酰支链淀粉并添加以修饰脂质体表面。测定修饰脂质体和常规脂质体的包封率、ζ电位、平均直径、跨距。采用反相高效液相色谱法测定小鼠组织中DIP的浓度。
修饰后，包封率降低，ζ电位升高，平均直径和跨距无明显变化。常规脂质体在肺、肝和脾中的DIP水平高于注射剂。与常规脂质体相比，修饰脂质体增加了肺中DIP的水平，降低了肝、脾中DIP的水平，而且延长了DIP在肺中的保留时间。
与常规脂质体和注射剂相比，修饰脂质体在小鼠体内的分布发生了显著变化。修饰脂质体具有明显的肺靶向性。
