人血浆蛋白多烯紫杉醇纳米粒子的自组装及对肿瘤的靶向性

Preparation and characterization of human serum albumin-docetaxel nanoparticles

目的：提高多烯紫杉醇的溶解度，提高其靶向性能。方法用二硫键断裂法制备人血清白蛋白多烯紫杉醇纳米粒子，并用电镜进行观察。对粒子载药量、稳定性及粒子对肿瘤部位趋向性进行表征。结果二硫键断裂法成功组装了白蛋白-多烯紫杉醇纳米粒子。电镜观察该纳米粒子外貌为80～100 nm左右的球形粒子，高效液相和蛋白质定量检测多烯紫杉醇载药量可达21．5％。结果白蛋白多烯紫杉醇纳米制剂可显著提高多烯紫杉醇的溶解度，提高对肿瘤靶向性。结论白蛋白-多烯紫杉醇纳米粒子对肿瘤细胞具有良好的靶向作用，具有临床运用的潜在价值。

Objective To improve the solubility of docetaxel and reduce its toxic and side effects, and to improve the targe-ting capability of docetaxel. Methods The human serum albumin-docetaxel nanoparticles were prepared by the disulfide bond reduction method, and were observed by electron microscope. The drug loading efficiency, stability and targeting capability of nanopar-ticles were explored. Results Albumin-docetaxel nanoparticles were successfully fabricated through disulfide bond reduction. Albumin-docetaxel nanoparticles were about 80-100 nm in diameter, and the loading of docetaxel was up to 21.5%. The marrow depression toxic-ity of albumin-docetaxel nanoparticles, which could accumulate at the tumor site, was reduced. Conclusion Albumin-docetaxel nano-particles have good targeting effect on tumor cells, which have potential value in clinical application.