叶酸修饰的长春新碱纳米脂质体的制备及其对人肝、肺癌细胞的作用
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篇名: 叶酸修饰的长春新碱纳米脂质体的制备及其对人肝、肺癌细胞的作用
TITLE:
摘要: 目的:制备叶酸(FA)修饰的长春新碱(VCR)纳米脂质体(VCR-nLip-FA)并考察其对人肝、肺癌细胞的作用。方法:采用硫酸铵梯度法制备VCR-nLip-FA,考察其粒径分布、Zeta电位、包封率、释放率。以人肝癌HepG2细胞、人肺癌A549细胞为例,比较VCR-nLip-FA和VCR-nLip的细胞摄取率和体外抑制效果(5~80 μg/ml)。结果:VCR-nLip-FA的粒径分布为98.1~159.0 nm,平均粒径为132.2 nm,平均Zeta电位为-40.1 mV,平均包封率为(86.6±3.5)%(n=4),24 h的累积释放率为(42.2±2.6)%。与VCR-nLip比较,A549细胞对VCR-nLip-FA的摄取率和VCR-nLip-FA对A549细胞活力的抑制作用差异无统计学意义(P>0.05);HepG2细胞对VCR-nLip-FA的摄取率和VCR-nLip-FA对HepG2细胞活力的抑制作用明显增加(P<0.01),且抑制作用呈浓度依赖性。结论:所制备的VCR-nLip-FA可高效地将抗癌药物靶向到HepG2细胞,并高效地抑制其生长;但对A549细胞的作用无明显提高。
ABSTRACT: OBJECTIVE: To prepare folic acid (FA)-loaded vincristine (VCR) nano liposome (VCR-nLip-FA) and to study its effects on human liver and lung cancer cells. METHODS: VCR-nLip-FA was prepared by ammonium sulfate gradient method, and particle size, Zeta-potential, encapsulation rate and release rate were investigated. Taking human liver cancer HepG2 cells and lung cancer A549 cells as example, uptake rate and inhibitory effect in vitro (5-80 μg/ml) were compared between VCR-nLip-FA and VCR-nLip. RESULTS: The particle size distribution, average particle size, average Zeta-potential, average encapsulation rate and 24 h accumulative release rate of VCR-nLip-FA were 98.1-159.0 nm, 132.2 nm, -40.1 mV, (86.6±3.5)% (n=4) and (42.2±2.6)%. Compared with VCR-nLip, there was no statistical significance in uptake rate of A549 cells to VCR-nLip-FA and inhibitory effect of VCR-nLip-FA on A549 cell viability (P>0.05); uptake rate of HepG2 cells to VCR-nLip-FA and inhibitory effect of VCR-nLip-FA on HepG2 cell viability increased significantly (P<0.01), in dose-dependent manner. CONCLUSIONS: Prepared VCR-nLip-FA can target anti-tumor drug to HepG2 cells efficiently, and highly inhibit the growth of HepG2 cells. But it has no higher effects on A549 cells.
期刊: 2016年第27卷第19期
作者: 寇卫政,杨晓煜,杨留中,杨丹,姬颖华
AUTHORS: KOU Weizheng,YANG Xiaoyu,YANG Liuzhong,YANG Dan,JI Yinghua
关键字: 叶酸修饰的长春新碱纳米脂质体;肝靶向性;肝癌HepG2细胞;肺癌A549细胞
KEYWORDS: Folic acid-loaded vincristine nano liposome; Liver-targeting; Liver cancer HepG2 cells; Lung cancer A549 cells
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