期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 405, 期 1-2, 页码 228-233出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2010.12.014
关键词
Stroke; Citicoline; CDP-choline; Liposomes; MRI
资金
- Spanish Ministry of Science and Innovation (MCIN) [SAF 2008-02190]
- Xunta de Galicia [INCITEO8PXIB927229PR]
- Institut de Salud Carlos III [CP09/00074, RETICS-RD06/0026]
Liposome encapsulation of active principles enhances their bioavailability to the brain. We investigated whether encapsulation of citicoline in liposomes increases its therapeutic effects in ischemia, performing a longitudinal MRI study of lesion volumes and edema in an animal model of stroke. Nineteen rats were submitted to permanent occlusion of the middle cerebral artery and treated with: (1) saline, (2) intraperitoneal citicoline (500 mg/kg), (3) intravenous citicoline (48 mg/kg), and (4) intravenous liposome-encapsulated citicoline (48 mg/kg). Lesion volumes were measured by MRI at days 0, 1, 3 and 7 following surgery. Encapsulation in liposomes increased the therapeutic effects of citicoline, as reflected by a 32% reduction of the infarct sizes at day 7, in contrast with controls where infarct sizes at day 7 increased by 39%, respect to values at day O. Intravenously injected citicoline reduced infarct sizes by 9% while intraperitoneal citicoline resulted in an increase of infarct sizes by 10%. A slight (not significant) reduction of edema formation was observed for animals treated with citicoline, in all of its delivery forms. Liposome-encapsulated citicoline causes a noticeable reduction in lesion volumes as compared to free citicoline (either i.p. or i.v.) at days 1,3 and 7 following permanent stroke. (C) 2011 Elsevier B.V. All rights reserved.
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