ZS-1多肽修饰载紫杉醇靶向脂质体抑制NCI-H1299肺癌细胞的研究

Inhibitory effect of ZS-1 modified paclitaxel liposome on lung cancer cell line NCI-H1299 in vitro

目的以人源性肺癌细胞NCI-H1299为模型,研究ZS-1多肽修饰的载紫杉醇脂质体(ZS-1 modified paclitaxel liposome,ZSLP-PTX)的体外抗肿瘤作用。方法采用薄膜分散法制备ZSLP-PTX,并对其理化性质进行表征。MTT实验研究ZSLP-PTX对NCI-H1299肿瘤细胞的增殖抑制能力,用定性和定量的细胞摄取实验研究ZS-1修饰脂质体与肺癌细胞的亲和力。构建NCI-H1299细胞肿瘤球模型,研究不同脂质体对肿瘤球的穿透能力。结果ZSLP-PTX的粒径为(125.7±18.5)nm,24小时内,在50%的血清中能保持稳定。NCI-H1299细胞和NCI-H1299体外肿瘤球对ZSLP的摄取能力大于LP-PTX(P<0.05);ZSLP-PTX对NCI-H1299细胞的增殖抑制作用显著强于LPPTX(P<0.05)。结论与LP-PTX比较,ZSLP-PTX能够更有效地被NCI-H1299肿瘤细胞所摄取,抑制肿瘤细胞的增殖,具有更强的抗肿瘤作用。

Objective To determine the effect of ZS-1 modified paclitaxel liposome （ZSLP-PTX） on lung cancer cell line NCI-H1299 in vitro. Methods ZSLP-PTX was prepared by film-ultrasonic method. The particle size,Zeta potential and stability in serum were evaluated. The uptake of ZSLP-PTX by NCI-H1299 cells in vitro and the penetration into tumor spheroids were examined. The anti-proliferation effect of ZSLP-PTX was evaluated by MTY assay. Results The average particle diameter of ZSLP-PTX was （ 125.7 ± 18.5 ） nm. The uptake of ZSLP-PTX by NCI-H1299 was significantly higher than that of LP-PTX（ P 〈 0.05 ）. Strong fluorescence intensity showed a deep penetration of ZSLP-PTX in tumor spheroids. The anti-proliferation effect of ZSLP-PTX was significantly greater than that of LP-PTX （ P 〈 0. 05 ）. Conclusion Compared to LP-PTX,ZSLP-PTX can penetrate into NCI-HI299 cells more effectively and exert a stronger antitumor effeet.