期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 72, 期 -, 页码 110-118出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.10.007
关键词
Cholesterylated glucosides; Brain targeting; GLUT1 transporter; Synthesis; Liposome
资金
- National Natural Science Foundation of China [81072532]
- Ph.D. Programs Foundation of Ministry of Education of China [20110181130011]
- Science & Technology Pillar Program of Sichuan Province of China [2011SZ0014]
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.
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