三氧化二砷白蛋白纳米微球的制备及体外释药特性  

Preparation and the release characteristic in vitro of arsenic trioxide albumin nanospheres

作　　者：周洁[1] 曾甫清[1] 高翔[2] 谢蜀生[2] 魏树礼[3] 

机构地区：[1]华中科技大学同济医学院附属协和医院泌尿外科,武汉430022 [2]北京大学医学部免疫药理室,北京100083 [3]北京大学药学院,北京100083

出　　处：《中国新药杂志》2005年第1期54-57,共4页Chinese Journal of New Drugs

基　　金：国家自然科学基金(39770739);国家青年自然科学基金(30200284)

摘　　要：目的:制备三氧化二砷白蛋白纳米微球(As_2O_3-BSA-NS)并鉴定其体外释放特性。方法:通过交联固化的方法制备三氧化二砷蛋白徽球。以粒子(粒径<1μm)分布百分数、载药量和包封率为指标设立总的优化指数(DF)。选择因素有油相/水相比、高速分散速度、BSA浓度和搅拌固化时间,按正交设计优化制备工艺。用体外释药方法研究其释放特性。结果:4个因素中,高速分散速度对总优化指数影响最大(P<0.01),其次是BSA浓度和油相/水相比(P<0.05),搅拌固化时间对指数几乎没有影响(P>0.05)。体外释药实验证实三氧化二砷蛋白微球释药速度明显慢于单纯的三氧化二砷。结论:使用优化的交联固化的方法可以制备出符合要求的三氧化二砷蛋白微球,其具有明显的缓释功能。Objective:To prepare and characterize arsenic trioxide albumin nanospheres (As_2O_3-BSA-NS). Methods: As_2O_3-BSA-NS was prepared by a chemical cross-inking technique. The optimal microsphere formulation was established based on the defined factors (DF) with the particle size (<1μm)distribution, loading dose and drug compounding efficiency. The final arsenic trioxide albumin nanospheres were prepared by an orthogonal manufacture protocol including W/O ratio, high distribution rate, BSA concentration and blending solidification time. The release of the As_2O_3 from the nanosphere was assessed by a dissolution test in vitro. Results:The study showed that the most factors to prepare the nanosphere is the distribution rate (P<0.01) and then BSA concentration as well as W/O ratio (P<0.05). The blending solidification time had not notable contributions on the defined factors (P>0.05). The slower sustained release of arsenic trioxide albumin nanosphere was attainable compared with the conventional dosage form of arsenic trioxide. Conclusion: The optimal As_2O_3-BSANS features the sustained release.

关 键 词：三氧化二砷 蛋白微球 制备 体外释药 

分 类 号：R979.19[医药卫生—药品] R737.14[医药卫生—药学]