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血脑屏障技术平台在预测各种化疗药物中枢神经系统渗透性方面的应用。2. 用于脑递送的阳离子肽载体。

Applications of a blood-brain barrier technology platform to predict CNS penetration of various chemotherapeutic agents. 2. Cationic peptide vectors for brain delivery.

作者信息

Adenot M, Merida P, Lahana R

机构信息

Synt:em, Nîmes, Paris, France.

出版信息

Chemotherapy. 2007;53(1):73-6. doi: 10.1159/000098422. Epub 2007 Jan 3.

Abstract

BACKGROUND

SynB family peptides conjugated to several drugs have been shown to increase the brain uptake and in vivo activities of these drugs via an adsorptive-mediated transcytosis mechanism. Based on both in vivo and in vitro experimental data, a cell uptake component has been added to our computational model of blood-brain barrier.

METHODS

In situ brain perfusion, in vitro cell model and a computational cell uptake model have been used to discover brain-penetrating properties of SynB peptides and to screen libraries of new rationally designed peptide vectors suitable for brain drug delivery.

RESULTS AND CONCLUSION

Starting from small peptide vectors that enhance the brain transport coefficient, the BBB platform has made it possible to design libraries of peptide vectors with enhanced transport properties.

摘要

背景

与多种药物偶联的SynB家族肽已被证明可通过吸附介导的转胞吞作用机制增加这些药物的脑摄取和体内活性。基于体内和体外实验数据,我们在血脑屏障计算模型中加入了细胞摄取成分。

方法

采用原位脑灌注、体外细胞模型和计算细胞摄取模型来发现SynB肽的脑穿透特性,并筛选适合脑药物递送的新的合理设计的肽载体文库。

结果与结论

从增强脑转运系数的小肽载体出发,血脑屏障平台使得设计具有增强转运特性的肽载体文库成为可能。

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