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首页> 外文期刊>Biomaterials >In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease
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In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease

机译：多奈哌齐缓释微粒在体外和体内的治疗阿尔茨海默氏病评估

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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.
机译：这项工作的目的是制备多奈哌齐微粒（DM），并评估其每月一次皮下注射作为缓释输送系统的优势。使用聚（D，L-丙交酯-共-乙交酯）（PLGA）通过油水乳液溶剂蒸发技术制备DM。 DM显示出加载率为13.2 +/- 2.1％（w / w），产率为54.8 +/- 0.8％，平均粒度为约75μm。 DM的体外释放表明多奈哌齐在水中28天内完全释放，但至磷酸盐释放盐水（PBS，pH 5.8）和PBS（pH 7.4）直至30天的累积释放百分比分别为98.4％和49.1％。体内实验表明，DM（90 mg / kg）在大鼠体内产生持续释放过程，并在第8天达到稳态浓度，并维持至第27天，多奈哌齐的稳态水平在130.3 +/- 7.8和121之间+/- 9.8 ng / ml，与通过口服途径给药的游离多奈哌齐（每天3 mg / kg）一致。通过皮下输注大鼠的DM（90 mg / kg）通过口服途径产生与游离多奈哌齐（3 mg / kg天）相同的药理作用。这些结果暗示DM作为持续释放递送策略可以代替其口服制剂用于AD疗法并实现每月一次的给药。 （c）2006 Elsevier Ltd.保留所有权利。

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