Abstract
A series of lactyl cholesterols as targeting liposome ligands for brain-specific delivery were synthesized. The lactic acid protected by benzyl group was coupled with cholesteryl oligoethylene carboxylate derivatives 3, then deprotected in tetrahydrofuran by Pd/C with H2 to obtain the title compounds La-Lf. As a model drug, tegafur was entrapped by liposmes and lipsomes coated with these ligands for in vivo study, which showed that the ligand could enhance the ability of liposome delivering tegafur across the blood-brain barrier.
Keywords: Liposome, Liposome ligands, Monocarboxylic acid transport, Tegafur, Blood-brain barrier, Brain targeting
Letters in Drug Design & Discovery
Title: Enhanced Brain Targeting of Tegafur Using Novel Lactyl Cholesterol Liposome as a Carrier
Volume: 6 Issue: 7
Author(s): Wei Fan, Xiankun Li, Shan Qian, Shan Wang and Yong Wu
Affiliation:
Keywords: Liposome, Liposome ligands, Monocarboxylic acid transport, Tegafur, Blood-brain barrier, Brain targeting
Abstract: A series of lactyl cholesterols as targeting liposome ligands for brain-specific delivery were synthesized. The lactic acid protected by benzyl group was coupled with cholesteryl oligoethylene carboxylate derivatives 3, then deprotected in tetrahydrofuran by Pd/C with H2 to obtain the title compounds La-Lf. As a model drug, tegafur was entrapped by liposmes and lipsomes coated with these ligands for in vivo study, which showed that the ligand could enhance the ability of liposome delivering tegafur across the blood-brain barrier.
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Cite this article as:
Fan Wei, Li Xiankun, Qian Shan, Wang Shan and Wu Yong, Enhanced Brain Targeting of Tegafur Using Novel Lactyl Cholesterol Liposome as a Carrier, Letters in Drug Design & Discovery 2009; 6 (7) . https://dx.doi.org/10.2174/157018009789108303
DOI https://dx.doi.org/10.2174/157018009789108303 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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