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目的探讨5-氟尿嘧啶聚乳酸载药纳米微粒(5-Fu-PLA-NP)对人胃癌和结肠癌细胞株的体外杀伤效应。方法超声乳化法制备5-Fu-PLA-NP载药纳米微粒;用噻唑蓝(MTT)比色法从1~10d连续检测1×10-7、1×10-6、1×10-5、1×10-4mol/L浓度5-Fu-PLA-NP和5-Fu对人胃癌细胞株MGC803和结肠癌细胞株SW620的体外杀伤效应,并计算出2种药物的半数抑制率浓度IC50和对肿瘤细胞的生长抑制率。结果5-Fu-PLA-NP的体外累积药物释放率在7d时为75.7%,10d时达94.3%;5-Fu的杀伤效应在1~7d时呈时间依赖关系,7d后进入平台期;5-Fu-PLA-NP则在1~10d均呈时间依赖关系;7d时两者在不同剂量的杀伤效应均呈剂量依赖关系,并且两者间差异无统计学意义。结论5-Fu-PLA-NP具有药物缓释效应,可延长药物对人胃癌与结肠癌细胞的有效作用时间;并且载药纳米微粒没有降低5-Fu成分的生物学活性。
Objective To investigate the in vitro killing effect of 5-fluorouracil-loaded polylactic acid-loaded nanoparticles (5-Fu-PLA-NP) on human gastric cancer and colon cancer cell lines. Methods 5-Fu-PLA-NP nanoparticles were prepared by phacoemulsification. The concentrations of 1 × 10-7, 1 × 10-6 and 1 × 10-5 were detected continuously by MTT assay from 1 to 10 days. In vitro killing effects of 5-Fu-PLA-NP and 5-Fu with 1 × 10-4 mol / L 5-Fu on human gastric cancer cell line MGC803 and colon cancer cell line SW620 were calculated and the IC50 of half-inhibitory rate Growth inhibition rate of tumor cells. Results The cumulative drug release rate of 5-Fu-PLA-NP in vitro was 75.7% at 7 days and 94.3% at 10 days. The killing effect of 5-Fu was in a time-dependent manner from 1 to 7 days and reached plateau after 7 days. 5 -Fu-PLA-NP showed a time-dependent relationship between 1 and 10 days. At 7 days, the cytotoxicity of the two drugs at different doses showed a dose-dependent manner, and there was no significant difference between them. CONCLUSION: 5-Fu-PLA-NP has the drug-releasing effect and prolongs the effective time of drugs on human gastric cancer and colon cancer cells. And the drug-loaded nanoparticles do not reduce the biological activity of 5-Fu.