125I-AIBZM Nanoliposomes  Targeting Brain as Imaging Agents

Abstract

Abstract: The aim of this study is to develop a blood brain barrier (BBB) 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 (~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 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 125I-AIBZM-Lf-L (p <0.01) but remarkably higher than that of 125I-AIBZM (p <0.01). Conclusion: 125I-AIBZM-Lf-L nano-liposome drug delivery system can increase the brain uptake of imaging agent 125I-AIBZM.

Key words: 125I, Dopamine D2 receptor, Lactoferrin, liposome, In vivo fluorescence imaging

CLC Number:

中图分类号 O628.5

TrendMD:

LI Guang-Hui, SHEN Hai-Xing, QIAN Jun, SI Zhan, ZHU Jian-Hua*. 125I-AIBZM Nanoliposomes Targeting Brain as Imaging Agents[J]. Chem. J. Chinese Universities, 2011, 32(6): 1295.

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125I-AIBZM Nanoliposomes Targeting Brain as Imaging Agents

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