中文摘要：

将苯甲酰胺类衍生物^125I-（S）-5-碘-N-（1-乙基-2-吡咯烷基）甲基-4-氨基-2-甲氧基苯酰胺（^125I-AIBZM）包载于具有脑靶向功能的纳米脂质体载药系统中,以提高^125I-AIBZM的入脑量.采用硫酸铵梯度主动载药法制备了^125I-AIBZM-脂质体（^125I-AIBZM-L）和^125I-AIBZM-Lf-脂质体（^125I-AIBZM-Lf-L）,脂质体形状规则,分布均匀,粒径在100 nm左右,两种脂质体的^125I-AIBZM包封率分别为39%和35%.包载荧光素DIR的DIR-脂质体（DIR-L）和DIR-Lf-脂质体（DIR-Lf-L）的小鼠荧光活体成像研究显示,DIR-Lf-L具有明显的脑靶向性,证实了乳铁蛋白（Lf）介导脑靶向的功能.药动力学实验表明,^125I-AIBZM-L与^125I-AIBZM-Lf-L在大鼠体内的血循环时间比^125I-AIBZM明显延长,各时相^125I-AIBZM-Lf-L的入脑量显著高于^125I-AIBZM-L（P〈0.01）,而125I-AIBZM-L的入脑量又显著高于^125I-AIBZM（P〈0.01）.

英文摘要：

The aim of this study is to develop a blood brain barrier permeable nano-liposome drug delivery system that significantly up-regulates the brain uptake of（S）-5-^125I-N-（1-ethyl-2-pyrrolidinyl）methyl-4-amine-2-methoxy-benzamide（^125I-AIBZM） as an imaging agent.Both 125I-AIBZM-nanoliposome（^125I-AIBZM-L） and ^125I-AIBZM-lactoferrin-nanoliposome（^125I-AIBZM-Lf-L） were prepared by the ammonium sulfate gradient method with a small particle size（ca.100 nm） and a narrow size distribution pattern.The encapsulation efficiencies of ^125I-AIBZM-L and 125I-AIBZM-Lf-L were measured as 39% and 35%,respectively.In vivo fluorescence imaging results showed that DIR-Lf-L was successfully delivered drug into the brain.The pharmacokinetic experiments in rats indicated that the blood circulation times of 125I-AIBZM-L and ^125I-AIBZM-Lf-L were substantially longer than that of small molecular 125I-AIBZM.Amount of intracerebral ^125I-AIBZM delivered by ^125I-AIBZM-L was significantly lower than that of ^125I-AIBZM-Lf-L（P〈0.01） but remarkably higher than that of ^125I-AIBZM（P〈0.01）.In conclusion,^125I-AIBZM-Lf-L nano-liposome drug delivery system can increase the brain uptake of imaging agent 125I-AIBZM.