氟尿嘧啶白蛋白磁性亚微球特性研究

 目的制备以牛血清白蛋白为载体的氟尿嘧啶白蛋白磁亚微球(FU-AMOM)并研究其有关特性。方法采用乳化-超声-固化法制备FU-AMOM并考察其外观、粒径及其分布;测定FU-AMOM的载药量及包封率;评价其释药特征并对释药曲线进行方程拟合;考察荷瘤小鼠体内靶向性。结果制得FU-AMOM平均粒径为(321±50)nm,分布范围为100～600nm;平均载药量为(9.69±0.19)%;平均包封率为(70.36±0.53)%;体外动态透析法释药模型符合Higuchi方程,具有明显的缓释作用;荷瘤小鼠试验结果表明,FU-AMOM于磁场作用下在肿瘤组织聚集,具有靶向性。结论FU-AMOM磁亚微球具有较好的缓释和靶向作用,有希望作为新型药物载体用于靶向给药系统。

Study on Properties in vitro of Fluorouracil Albumin Magnetic Deuto-Microspheres

OBJECTIVE To prepare bovine serum albumin magnetic deuto-microspheres of fluorouracil(FU-AMDM) and study their properties.METHODS The magnetic deuto-microspheres were prepared by emulsion-ultrasound-heat stabilization techniques.The shape and size distribution were observed. High-performance liquid chromatography was used to determine the content of fluorouracil. The release test of FU from AMDM in vitro was carried out by using constant temperature vibration dialysis assay.The targeting property was studied in tumor-bearing mice. RESULTS The mean diameter of FU-AMDM was (321±50)nm,with the range from 100 nm to 600 nm. The drug loading and drug trapping efficiency of FU-AMDM were (9.69±0.19)% and (70.36±0.53)%,respectively. The drug release profile was described by Higuchi equation. The drug concentration in tumor tissues was higher than other sites. CONCLUSION FU-AMDM has potential prospects in sustained release and targeted localization,and will be used in targeting drug delivery system.