CDP-choline liposomes provide significant reduction in infarction over free CDP-choline in stroke
CDP-choline liposomes provide significant reduction in infarction over free CDP-choline in stroke
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DOI：
10.1016/j.brainres.2005.07.067
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发表时间：
2005-10-05
期刊：
影响因子：
2.9
通讯作者：
Tureyen, K
中科院分区：
文献类型：
--
作者：
Adibhatla, RM;Hatcher, JF;Tureyen, K
Cytidine-5' -diphosphocholine (CDP-choline, Citicoline, Somazina) is in clinical use (intravenous administration) for stroke treatment in Europe and Japan, while USA phase III stroke clinical trials (oral administration) were disappointing. Others showed that CDP-choline liposomes significantly increased brain uptake over the free drug in cerebral ischemia models. Liposomes were formulated as DPPC, DPPS, cholesterol, GM(1) ganglioside; 7/4/7/1.57 molar ratio or 35.8/20.4/35.8/8.0 mol%. GM(1) ganglioside confers long-circulating properties to the liposomes by suppressing phagocytosis. CDP-choline liposomes deliver the agent intact to the brain, circumventing the rate-limiting, cytidine triphosphate:phosphocholine cytidylyltransferase in phosphatidylcholine synthesis. Our data show that CDP-choline liposomes significantly (P < 0.01) decreased cerebral infarction (by 62%) compared to the equivalent dose of free CDP-choline (by 26%) after I h focal cerebral ischemia and 24 h reperfusion in spontaneously hypertensive rats. Beneficial effects of CDP-choline liposomes in stroke may derive from a synergistic effect between the phospholipid components of the liposomes and the encapsulated CDP-choline. (c) 2005 Elsevier B.V. All rights reserved.
