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

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。

Preparation and characterization of human serum albumin-docetaxel nanoparticles

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.