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.