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目的研究用半乳糖脂修饰的脂质体与肝特异性半乳糖受体结合的能力,为用该脂质体包埋药物进行肝病治疗和肝造影提供依据。方法半乳糖经乙酰化、溴化、缩合、亲核取代反应制备半乳糖新糖脂质并与其他脂质制备脂质体,在二氯化锡还原作用下用99mTc标记脂质体,进行动物体内靶肝实验,用γ计数器检测各脏器放射性,计算摄取率。结果标记脂质体的标记率大于95%,动物体内实验肝最大摄取率为801%,对照组为315%。乳糖封闭受体后,肝摄取率明显下降(321%),差异有显著意义(t=522,P<001)。结论半乳糖脂修饰的脂质体具有很好的靶肝作用,这种靶向性是与肝半乳糖受体结合的结果。
Objective To study the ability of galactolipid-modified liposomes to bind with liver-specific galactose receptor, and to provide a basis for liver drug therapy and hepatic angiography using drug-loaded liposomes. Methods The galactose liposomes were prepared by acetylation, bromination, condensation and nucleophilic substitution reaction of galactose and liposomes were prepared with other lipids. The liposomes were labeled with 99mTc under the action of tin dichloride reduction, In vivo target liver experiments, γ counters were used to measure the radioactivity of various organs and the uptake was calculated. Results The labeling rate of liposomes was more than 95%. The maximum uptake rate of experimental liver in animals was 801% and that of control group was 315%. Lactose blocked receptor, the liver uptake rate decreased significantly (32 1%), the difference was significant (t = 5 22, P <0 01). Conclusion The galactolipid-modified liposomes have good target liver function, which is the result of binding to hepatic galactose receptor.