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以转铁蛋白溶液为外水相,纳米沉淀技术制备了表面含转铁蛋白的包载卡莫司汀的聚乳酸纳米微粒,药物释放时间达一周以上。体外细胞实验验证纳米微粒表面转铁蛋白保持了活性,纳米粒子与胶质瘤细胞具有较强的结合能力。立体定位注射纳米微粒至荷瘤鼠瘤腔,SPECT考察载药纳米微粒的体内分布,表明纳米微粒在颅内滞留。与对照组相比,注射载药纳米微粒的大鼠生存期显著延长,核磁共振图象显示其中2只大鼠颅内肿瘤消退,表明载药纳米粒子对恶性胶质瘤具有体内抑制作用。
The transferrin-coated polylactic acid nanoparticles containing transferrin were prepared by using transferrin solution as outer aqueous phase and nano-precipitation technique. The drug release time was more than one week. In vitro experiments showed that the transferrin on the surface of nanoparticles retained the activity, and nanoparticles had strong binding ability with glioma cells. Stereotaxic injection of nanoparticles into the tumor-bearing rat tumor cavity, SPECT examination of drug-loaded nanoparticles in vivo distribution, indicating that nano-particles in the brain retention. Compared with the control group, the survival time of rats injected with drug-loaded nanoparticles was significantly prolonged, and nuclear magnetic resonance imaging showed the regression of the intracranial tumors in two of the rats, indicating that the drug-loaded nanoparticles have an in vivo inhibitory effect on the malignant glioma.