美斯地浓聚乳酸载药纳米粒的制备及体外释放  

Preparation and in vitro release of Mestinon-poly(lactic acid) nanoparticles

作　　者：徐美玲[1] 杨林 廖红[1] 胡雪原[1] 张景勍[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室,重庆市400016 [2]重庆市食品药品检验所,重庆市401121

出　　处：《中国组织工程研究》2013年第8期1384-1389,共6页Chinese Journal of Tissue Engineering Research

摘　　要：背景:美斯地浓临床常用于治疗重症肌无力,但其水溶性较强,半衰期短,生物利用度低,给药频率高,患者依从性差,因此提高其缓释作用对临床应用有重要意义。目的:制备美斯地浓聚乳酸纳米粒,并考察其体外释放性能。方法:以聚乳酸为载药材料,采用复乳液中干燥法制备美斯地浓聚乳酸纳米粒,运用单因素实验设计优化处方,动态透析法进行体外药物释放实验。结果与结论:确定以二氯甲烷作为油相制备纳米粒,内水相与油相的比例1:10,聚乳酸浓度6%,外水相聚乙烯醇浓度3%,美斯地浓投药量40mg为最佳制备工艺,此条件制备的药物纳米粒包封率和载药率分别为(67.59±1.46)%和(4.31±0.17)%。美斯地浓聚乳酸纳米粒的平均粒径为937nm,圆球形,表面光滑,未观察到粘连现象。与美斯地浓游离药物相比,美斯地浓聚乳酸纳米粒存在突释现象,之后呈现缓慢释放特性,72h释放量为57.03%,提示成功制备美斯地浓聚乳酸纳米粒,具有缓释效应。BACKGROUND： Mestinon has been used for the symptomatic treatment of myasthenia gravis. It is very soluble in water, which may be responsible for the short half-life and poor bioavailability. The high dosing frequency may cause poor patient compliance. It is of great clinical significance to develop a Mestinon sustained release delivery system. OBJECTIVE： To prepare a Mestinon-poly（lactic acid） nanoparticle and to assess its in vitro release characteristics.METHODS： Mestinon-poly（lactic acid） nanoparticle was prepared by a double emulsion-solvent evaporation method. Poly（lactic acid） was used as the carrier material. The single factor experiment was carried out to properly formulate Mestinon-poly（lactic acid） nanoparticle. The in vitro release test was investigated by a dialysis method. RESULTS AND CONCLUSION： The optimized conditions to prepare Mestinon-poly（lactic acid） nanoparticle were listed as follows： Dichioromethane was used as oil phase, the ratio between inner water phase and oil phase was 1：10, the poly（cactic acid） concentration was 6%, the polyvinyl alcohol concentration was 3%, and the amount of Mestinon was 40 mg. Mestinon-poly（lactic acid） nanoparticle prepared under the optimized conditions had an average particle size of 937 nm, an encapsulation efficiency of （67.59±1.46）% and a drug loading rate of （4.31 ±0.17）%. Mestinon-poly（lactic acid） nanoparticle displayed spherical shape with smooth surface and no aggregation was observed. Compared with free Mestinon, Mestinon-poly（lactic acid） nanoparticle had an initial burst release and subsequently a very slow release. The accumulated release rate of Mestinon-poly（lactic acid） nanoparticle was 57.03% at 72 hours. Mestinon-poly（lactic acid） nanoparticle with the good sustained-release characteristics could be successfully prepared.

关 键 词：生物材料 纳米生物材料 生物材料与药物控释 纳米粒 美斯地浓 聚乳酸 体外药物释放 单因素 实验 缓释 生物材料图片文章 

分 类 号：R318[医药卫生—生物医学工程]