三氧化二砷纳米微粒的制备及体外释药特性  

Preparation of As2O3nanoparticles and its drug release characteristics in vitro

作　　者：徐丽姝[1,2] 刘建化[1,2] 林萍[1,2] 黄开红[3] 陈茵婷[3] 陈其奎[3] 

机构地区：[1]广东省医学科学院 [2]广东省人民医院东病区消化科,广东广州510080 [3]中山大学附属第二医院消化内科,广东广州510120

出　　处：《南方医科大学学报》2010年第8期1790-1792,共3页Journal of Southern Medical University

基　　金：国家自然科学基金(30670951);广东省自然科学基金(06021322);广州市科技攻关项目(2003Z3-E0381);广东省科技攻关项目(2005B31211002);广东省教育部产学研结合项目(2009B090300277)

摘　　要：目的对聚乳酸载药纳米微粒的表面形貌、粒径分布、微粒结构、表面元素、体外释放等微粒性能进行考察与评价。方法以可溶性乳酸羟基乙酸共聚物(PLGA)为载体,三氧化二砷(As2O3)为模型药物,采用超声乳化法制备PLGA载As2O3纳米微粒(As2O3-NPS),通过电子显微镜观测纳米粒外形结构,用紫外分光光度计测得载纳米粒载药量包封率并测定体外释放量,用光电能谱仪测定纳米微粒表面元素。结果 As2O3-NPS呈规则球形,平均粒径(210±23)nm,测得载药量为29.6%,包封率为82.1%。体外释放实验表明纳米微粒具有缓释特性。结论以As2O3-NPS作为As2O3载体,可改变As2O3在体内的药代动力学行为,具有缓释作用,可制备为静脉用药,延长药物在体内的循环时间,发挥更好的抗肿瘤效应。Objective To prepare arsenic trioxide （As2O3）-loaded biodegradable polylactic-co-glycolic acid （PLGA） nanoparticles （NPS） and evaluate the glomcration ability, appearance, structure, surface and release characteristics of the NPs. Method With PLGA as the carrier material, As2O3 NPs （As2O3-NPS） were prepared with the method of matrix and ultrasound emulsification. According to the criteria of the diameter of the NPs, drug loading （DL） and embedding ratio （ER）, the process of NP preparation was optimized by scanning electron microscopy （SEM）, ultraviolet spectroscopy （UV）, and XPS. Results The As203-NPS prepared were uniformly spherical with an average diameter of 210±23 nm, DL of 29.6% and ER of 82.1%. The drug release assay in vitro showed a sustained drug-release capacity of the preparation. Conclusion As2O3-NPS may serve as a carrier of As2O3 to change the pharmacokinetics of As2O3 in vivo, allow slow drug release, and prolong the drug circulation time after intravenous injection, thereby producing better antitumor effects.

关 键 词：纳米微粒 三氧化二砷 乳酸羟基乙酸共聚物 缓释作用 

分 类 号：R944[医药卫生—药剂学]