磁性聚乳酸-羟基乙酸氧化酚砷纳米微粒的制备及其特性(英文)  

Preparation and characterization of magnetic poly D, L- lactide -co-glycolic acid phenylarsine oxide nanoparticles

作　　者：蔡晨[1] 董勤[2] 蔡洪培[2] 高申[3] 

机构地区：[1]解放军第二军医大学长海医院特诊科,上海市200433 [2]解放军第二军医大学长征医院消化科,上海市200003 [3]解放军第二军医大学药学院药剂学教研室,上海市200433

出　　处：《中国组织工程研究与临床康复》2008年第6期1140-1144,共5页Journal of Clinical Rehabilitative Tissue Engineering Research

基　　金：国家自然科学基金(30370644);上海科委纳米专项基金(0352nm107)~~

摘　　要：背景:基于纳米技术发展起来的纳米载体介导的磁性载药系统,在外加磁场作用下,能实现位点特异性靶向给药的目的,有利于提高病灶部位的局部药物浓度,从而进一步提高治疗效果,减少全身毒副作用。目的:研究磁性聚乳酸-羟基乙酸氧化酚砷纳米微粒的制备工艺,评价纳米粒子特性。设计:首先选择几个可能影响纳米微粒特性的因素进行了单因素实验,然后再根据实验结果,结合统计学中的正交设计,获得了最佳优化处方。单位:解放军第二军医大学长海医院特诊科。材料:实验于2005-01/2006-03在解放军第二军医大学药学院药剂教研室完成。实验用氧化酚砷购自美国Sigma公司,聚乳酸-羟基乙酸由山东医疗器械研究所提供,纳米级四氧化三铁购自美国Sigma公司,聚乙烯醇购自北京有机化工厂,二氯甲烷等其他试剂均为分析纯,购于上海国药集团化学试剂有限公司。方法:运用超声乳化-溶剂挥发法制备磁性聚乳酸-羟基乙酸氧化酚砷纳米微粒,通过透射电镜观察微粒形态,振动样品磁强计确证纳米微粒磁性的存在,激光粒径仪测定纳米粒的粒径大小和分布,高效液相法测定氧化酚砷的载药量及包封率,并计算氧化酚砷体外释放百分率。主要观察指标:磁性聚乳酸-羟基乙酸氧化酚砷纳米微粒的形态、粒径、载药量、包封率、磁性及体外释放情况。结果:①微粒包封率和载药量:实验制备的纳米粒平均包封率为34.2%;5批纳米粒载药量分别为3.06%,3.15%,3.18%,3.21%,3.41%,平均载药量为3.20%,批间差异较小,说明工艺稳定性、重现性好。②微粒形态:纳米微粒呈圆形,表面光滑,分布均匀,不粘连,磁性微球中可见非均匀分散的黑色不透光区,为四氧化三铁微粒。③微粒粒径:分布范围窄(140～500nm),平均290nm。④微粒磁性:在不断改变外加磁场的大小与方向的情况下,微粒具有不同的磁化强度,说明氧BACKGROUND： With the development of nanotechnology, a new system for the delivery of drugs by magnetic nanovectors has been proposed. Within a magnetic field, the system can implement site-specific drug administration, thereby raising drug concentration at the lesion focus, elevate therapeutic effects, and reduce side effects. OBJECTIVE： To study the preparation of magnetic poly D, L-lactide-co-glycolic acid phenylarsine oxide nanoparticles （M-PLGA-PAO-NPs） and to evaluate characteristics of the prepared nanoparticles. DESIGN： Several factors influencing nanoparticle characteristics were selected for single-factor tests. Then, according to experimental results, and in conjunction with orthogonally designed statistics, the optimized prescription was obtained. SETTING： Department of Special Diagnosis, Changhai Hospital, Second Military Medical University of Chinese PLA. MATERIALS： The study was performed at the Department of Pharmaceutics, School of Pharmacy, Second Military Medical University of Chinese PLA from January 2005 to March 2006. The reagents used were as follows： phenylarsine oxide （Sigma, USA）, poly D, L-lactic-co-glycolic acid （Shandong Medical Apparatus Institute, China）, ferroso-ferric oxide （nanometer, Sigma, USA）, polyvinyl alcohol （PVA1788, Beijing Organic Chemical Industry Plant, China）. Methylene dichloride and other agents were all analytical grade and purchased from Shanghai Sinopharm Chemical Reagent Co., Ltd, China. METHODS： M-PLGA-PAO-NPs were prepared through an emulsion-evaporation process. Nanoparticle shape was observed by transmission electron microscopy. Magnetism was determined by a vibrating sample magnetometer. The size and diametral distribution of nanoparticles were determined by a laser particle size analyzer. The encapsulation ratio and drug loading of phenylarsine were measured by high performance liquid chromatography （HPLC）. The percentage of phenylarsine oxide release in vitro was calculated [the percentage of phenylarsine oxide releas

关 键 词：纳米粒 氧化酚砷 聚乳酸-羟基乙酸 磁性 

分 类 号：R318.08[医药卫生—生物医学工程]