【摘要】 目的探讨聚乙二醇相对分子质量对载羟喜树碱(HCPT)的聚乙二醇化聚十六烷基氰基丙烯酸酯纳米囊泡(PEG-PHDCA)在S180肉瘤小鼠体内的肿瘤靶向性及抗肿瘤作用的影响。方法选用司盘60和PEG-PHDCA为载体材料,制备HCPT的PEG-PHDCA隐形纳米囊泡,进行S180肉瘤小鼠瘤内药动学试验和抑瘤试验。结果PEG相对分子质量为2 000、5 000、10 000的PEG-PHDCA纳米囊泡在S180肉瘤小鼠肿瘤中125I-HCPT的AUC分别为HCPT的9.21、13.82、9.48倍;对S180肉瘤小鼠抑瘤率分别为88%、97.1%、80.8%,普通纳米粒PHDCA组抑瘤率为41.8,而原药组抑瘤率仅为17.3%。结论PEG修饰纳米囊泡明显优于原药和未经PEG修饰纳米囊泡,PEG相对分子质量为5 000,粒径为80 nm左右时,载HCPT的隐形纳米囊泡具有最佳肿瘤靶向作用。更多还原

【Abstract】 AIM To investigate the tumor targeting effect and anti-tumor activity of hydroxycamptothecin(HCPT) loaded poly(methoxy-polyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate)(PEG-PHDCA) niosomes with different polyethylene glycol(PEG) chain length.METHODS Stealth PEG-PHDCA niosomes were prepared with span60 and PEG-PHDCA acting as drug carrier.S180 tumor bearing mice were used for biodistribution test and anti-tumor test.RESULTS Niosomes with PEG chain length of 2 000,5 000,10 000 showed an obvious tumor targeting effect,with AUC in tumor increasing by 9.21,13.82 and 9.48-fold,respectively,compared with HCPT.The tumor inhibition rate of niosomes with PEG chain length of 5 000,2 000,10 000 were 88%,97.1%,80.8%,respectively,while HCPT had only 17.3% inhibition rate.CONCLUSION PEG-PHDCA niosomes have a better anti-tumor effect than HCPT and PHDCA niosomes.Under this experimental conditions,PEG-PHDCA niosomes with PEG chain length of 5 000 and particle size of 80 nm have the most significant tumor targeting effect.更多还原