In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease
文献类型：期刊论文
| 作者 | Zhang, Pengcheng ; Chen, Lingli; Gu, Wangwen; Xu, Zhenghong; Gao, Yu; Li, Yaping
|
| 刊名 | BIOMATERIALS
 |
| 出版日期 | 2007-04 |
| 卷号 | 28期号:10页码:1882-1888 |
| 关键词 | donepezil PLGA microparticles acetylcholinesterase inhibitor sustained release |
| ISSN号 | 0142-9612 |
| DOI | 10.1016/j.biomaterials.2006.12.016 |
| 文献子类 | Article |
| 英文摘要 | The purpose of this work is to prepare donepezil microparticles (DM) and evaluate its advantage as a sustained release delivery system with subcutaneous injection once a month. DM was prepared using poly (D,L-lactide-co-glycolide) (PLGA) by an oil-water emulsion solvent evaporation technique. DM showed the loading ratio 13.2 +/- 2.1% (w/w) and yield 54.8 +/- 0.8% with mean particle size about 75 pm. In vitro release of DM showed that donepezil completely released within 28 days in water, but the cumulative release percentages up to day 30 were 98.4% and 49.1% for phosphate buffer saline (PBS, pH 5.8) and PBS (pH 7.4), respectively. The in vivo experiment demonstrated that DM (90 mg/kg) produced a sustained release process in rats, and reached steady-state concentration at day 8 and maintained until day 27 with steady-state levels of donepezil between 130.3 +/- 7.8 and 121 +/- 9.8 ng/ml, which was accordance with that of free donepezil by oral application route (3 mg/kg day). DM (90 mg/kg) by subcutaneous infusion in rats produced the same pharmacological role as free donepezil (3 mg/kg day) by oral application route. These results implicated that DM as a sustained release delivery strategy could substitute for its oral formulation for therapy of AD and come true its administration once a month. (c) 2006 Elsevier Ltd. All rights reserved. |
| WOS关键词 | CHOLINESTERASE ACTIVITY ; HYDROCHLORIDE E2020 ; RATS ; MICROSPHERES ; MEMORY |
| WOS研究方向 | Engineering ; Materials Science |
| 语种 | 英语 |
| WOS记录号 | WOS:000244436000015 |
| 出版者 | ELSEVIER SCI LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273289]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Li, Yaping |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Pengcheng,Chen, Lingli,Gu, Wangwen,et al. In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease[J]. BIOMATERIALS,2007,28(10):1882-1888. |
| APA | Zhang, Pengcheng,Chen, Lingli,Gu, Wangwen,Xu, Zhenghong,Gao, Yu,&Li, Yaping.(2007).In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease.BIOMATERIALS,28(10),1882-1888. |
| MLA | Zhang, Pengcheng,et al."In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease".BIOMATERIALS 28.10(2007):1882-1888. |
入库方式： OAI收割
来源：上海药物研究所
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