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合成了具有隐形及靶向肿瘤组织功能的NGR多肽衍生物,并用基质辅助激光解析电离飞行时间质谱进行了表征。采用硫酸铵梯度法制备了用不同比例NGR多肽衍生物修饰的马钱子碱脂质体,考察了所得制品在大鼠空白血浆中的体外释放情况。结果表明,NGR多肽衍生物修饰的脂质体体外释放速率比未修饰脂质体慢。测定了马钱子碱溶液及不同处方脂质体分别以5 mg/kg的剂量经静脉给予大鼠后的血药浓度。药动学结果显示,脂质体组AUC是溶液组的5~6倍,与普通隐形脂质体组相比,仅加入1.28%NGR多肽衍生物的脂质体组MRT显著延长,其他药动学参数没有显著差异。
NGR polypeptide derivatives with invisible and tumor-targeted functions were synthesized and characterized using matrix-assisted laser desorption / ionization time-of-flight mass spectrometry. The strychnine liposomes modified with different ratios of NGR polypeptide derivatives were prepared by ammonium sulfate gradient method and the in vitro release of the obtained products in blank plasma of rats was investigated. The results showed that the NGR polypeptide derivative modified liposome release rate in vitro than the unmodified liposomes slower. The blood concentration of strychnine solution and different prescription liposomes were measured after intravenous administration of 5 mg / kg rat. Pharmacokinetic results showed that the AUC of the liposome group was 5 to 6 times higher than that of the solution group. Compared with the common invisible liposome group, the MRT of the liposome group containing only 1.28% of the NGR polypeptide derivative was significantly prolonged. Other pharmacokinetics There is no significant difference in learning parameters.