Design, synthesis and biological evaluation of multivalent glucosides with high affinity as ligands for brain targeting liposomes
Design, synthesis and biological evaluation of multivalent glucosides with high affinity as ligands for brain targeting liposomes
复制标题
具有高亲和力的多价糖苷作为脑靶向脂质体配体的设计、合成和生物学评价。
DOI：
10.1016/j.ejmech.2013.10.007
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发表时间：
2014-01-24
影响因子：
6.7
通讯作者：
Wu, Yong
中科院分区：
文献类型：
--
作者：
Qu, Boyi;Li, Xiaocen;Wu, Yong
设计并合成了新型双功能簇苷作为脂质体配体，用于制备新型脂质体，以实现GLUT1将药物制剂有效递送至大脑。成功制备了负载多西紫杉醇的五种脂质体并进行了动物试验。静脉注射后体内分布研究的结果这五种脂质体和空白多西紫杉醇的给药表明，偶联的脂质体Lip-1、Lip-2、Lip-3、Lip-5表现出优异的跨BBB转运能力。特别是，与空白多西紫杉醇和 Lip 相比，它们显着增加了大脑中多西紫杉醇的水平。其中，Lip-5表现出较高的脑浓度。小鼠体内的药代动力学和分布研究均证实，这种新型脑靶向药物递送系统是增强中枢神经系统药物脑部递送能力的有前途的载体。 (C) 2013 Elsevier Masson SAS。版权所有。
The new bifunctional cluster glucosides were designed and synthesized as liposome ligands for preparing novel liposome to achieve the effective delivery of drug formulations to brain by GLUT1. Docetaxel-loaded five liposomes were prepared successfully and tested in the animals. Results from the in vivo distribution study after i.v. administration of these five liposomes and blank-docetaxel indicated that the coupled liposomes Lip-1, Lip-2, Lip-3, Lip-5 exhibited excellent transport ability across the BBB. In particular, they significantly increased the level of docetaxel in brain compared to blank-docetaxel and Lip. Among them, Lip-5 showed higher brain concentration. Both pharmacokinetics and distribution study in mice confirmed that this novel brain targeting drug delivery system was a promising carrier to enhance brain delivery capacity for CNS drugs. (C) 2013 Elsevier Masson SAS. All rights reserved.