【作者】 罗斌华； 赵智卉； 丁红； 赵志娟；

【Author】 LUO Bin-hua1,2,ZHAO Zhi-hui1,DING Hong1,ZHAO Zhi-juan1 (1.Dept of Pharmaceutics,Shanxi Medical University,Shanxi Taiyuan 030001,China; 2.Dept of Pharmaceutics,Xianning University,Hubei Xianning 437100,China)

【机构】 山西医科大学药学院； 湖北咸宁学院药学院；

【摘要】 目的制备肺靶向阿霉素(ADM)-乳酸-羟基乙酸共聚物(PLGA)微球并考察其肺靶向特性。方法利用乳化溶剂扩散-吸附法制备肺靶向的ADM-PLGA微球。用反相高效液相色谱法测定给药后小鼠体内各组织中的药物浓度。结果制备的微球外观圆整,表面带正电荷,粒径范围在5～20μm占90.1%,载药量为5.93%,休止角θ≤30°,堆密度ρ=145.7±6.5mg?mL-1,体外释药速率符合Higuchi方程。小鼠尾静脉给药后,ADM-PLGA微球对靶部位有较好的选择性,相对于其他组织器官肺的te值增强2.7~4.5倍。结论采用乳化溶剂扩散-吸附法制备的ADM-PLGA微球具有较高的载药量,药物在小鼠肺部的分布优于阿霉素注射液,能达到肺靶向的目的。更多还原

【Abstract】 OBJECTIVE To prepare lung targeting ADM-PLGA microspheres and investigate their characteristics. METHODS ADM-PLGA microspheres were prepared by emulsion solvent diffusion-adsorbed method. HPLC method was established and validated for the determination of adriamycin in tissues of mice. RESULTS ADM-PLGA microspheres were spherical and regular in morphology, the particle size ranging from 5 to 20 μm accounted for 90.1%, the loading amount was 5.93%, angle of repose θ≤30°, bulk density ρ was 145.7±6.5 mg?mL-1,The release in vitro was characterized by Higuchi equation. Adriamycin PLGA microspheres and free adriamycin solution were injected intravenously at a dose of 5 mg?kg-1 to mice. Compared with solution, there was higher selective on the lung for microspheres. Compared with other organs, te value of the lung was increased by 2.7~4.5 times. CONCLUSION The loading amount is higher. The ADM-PLGA microspheres are regarded as showing more notable targeting efficacy than free adriamycin solution on the lung in mice.更多还原