Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain

被引:59
作者
Dufes, C
Gaillard, F
Uchegbu, IF
Schätzlein, AG
Olivier, JC
Muller, JM
机构
[1] Univ Poitiers, Fac Sci, CNRS, UMR 6558,LBSC,Equipe Biol Interact Cellulaires, F-86022 Poitiers, France
[2] Univ Glasgow, Canc Res UK Dept Med Oncol, Glasgow G61 1BD, Lanark, Scotland
[3] Univ Poitiers, Fac Sci, CNRS, UMR 6558,LBSC,Equipe Dev Cort, F-86022 Poitiers, France
[4] Univ Strathclyde, Strathclyde Inst Biomed Sci, Dept Pharmaceut Sci, Glasgow G4 0NR, Lanark, Scotland
[5] Fac Med & Pharm, Pharm Galen & Biopharm Lab, Equipe Emergente Medicaments Antiinfectieux & Bar, F-86005 Poitiers, France
关键词
niosomes; glucose; vasoactive intestinal peptide (VIP); brain delivery; blood-brain barrier;
D O I
10.1016/j.ijpharm.2004.07.020
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to evaluate glucose-bearing niosomes as a brain targeted delivery system for the vasoactive intestinal peptide (VIP). To this end, VIP/I-125-VIP-loaded glucose-bearing niosomes were intravenously injected to mice. Brain uptake was determined by measuring the radioactivity of I-125-labeled VIP using gamma-counting, after intravenous administration of VIP in solution or encapsulated in glucose-bearing niosomes or in control niosomes. VIP integrity was assessed by reversed-phase HPLC analysis of brain extracts. Distribution of I-125-VIP derived radioactivity was examined from serial brain slices. HPLC analysis confirmed the presence of intact VIP in brain after administration of VIP-loaded niosomes, but not after administration of VIP solution. Encapsulation within glucose-bearing niosomes mainly allowed a significantly higher VIP brain uptake compared to control niosomes (up to 86%, 5 min after treatment). Brain distribution of intact VIP after injection of glucose-bearing niosomes, indicated that radioactivity was preferentially located in the posterior and the anterior parts of the brain, whereas it was homogeneously distributed in the whole brain after the administration of control vesicles. In conclusion, this novel vesicular formulation of VIP delivers intact VIP to particular brain regions in mice. Glucose-bearing vesicles might be therefore a novel tool to deliver drugs across the blood-brain barrier (131313). (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码:77 / 85
页数:9
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