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本文采用了高压乳匀法制备载多烯紫杉醇白蛋白纳米粒,以期改善目前临床上多烯紫杉醇注射液的不良反应。考察了多烯紫杉醇白蛋白纳米粒的粒径、电位、包封率,并采用X射线衍射技术对多烯紫杉醇在纳米粒中的存在形式进行考察,还评价了多烯紫杉醇纳米粒的溶血性,药动学和药效学行为,以市售静注用多烯紫杉醇溶液(泰素帝)作为参比制剂。研究结果表明,多烯紫杉醇白蛋白纳米粒粒径(193±4)nm,电位(-30±1)mV和包封率为69%±2%,纳米粒冻干后具有良好的稳定性。与多烯紫杉醇溶液相比,白蛋白纳米粒制剂的溶血性有非常显著的改善(P<0.01),而药动学和抗肿瘤药效学方面两者较为相似。由此可见,白蛋白纳米粒将可作多西紫杉醇药物体内静脉注射用的安全有效载体。
In this paper, the preparation of docetaxel albumin nanoparticles loaded with high-pressure homogenization method, in order to improve the clinical adverse effects of docetaxel injection. The particle size, potential and encapsulation efficiency of docetaxel albumin nanoparticles were investigated. The existence of docetaxel in the nanoparticles was investigated by X-ray diffraction. The hemolytic activity of docetaxel nanoparticles , Pharmacokinetics and pharmacodynamic behavior, intravenous injection with docetaxel solution (Taxol) as a reference preparation. The results showed that the particle size of docetaxel albumin nanoparticles was (193 ± 4) nm, the potential (-30 ± 1) mV and encapsulation efficiency were 69% ± 2%. The nanoparticles had good stability after lyophilization. Compared with docetaxel solution, the hemolysis of albumin nanoparticle preparation had a very significant improvement (P <0.01), while the pharmacokinetics and antitumor pharmacodynamics were similar. Thus, albumin nanoparticles will be able to do docetaxel drug intravenous injection of safe and effective carrier.