Vascular endothelial growth factor receptor (VEGFR) is over-expressed on a variety of tumour cells and tumour neovasculature, and so becomes well-documented target for cancer treatment. This study was designed to evaluate the cellular targeting and anti-tumor potency of VEGF-conjugated nanoparticles (VEGF-NPs). The poly-lactic-co-glycolic acid nanoparticles were prepared using the emulsion-solvent evaporation method and the VEGF was conjugated on surface of nanoparticles by covalent coupling method. The obtained particles were found to be of spherical shape exhibiting a size of 710nm and VEGF conjugation efficiency was 16.6%. The results in vitro test showed that VEGF-NPs were more associated to Human Umbilical Vein Endothelial Cells by binding to VEGFR. In vitro cell proliferation test, IC50 showed the superior antiproliferative activity of paclitaxel-loaded VEGF-NPs over unconjugated nanoparticles and native paclitaxel due to higher cellular association on tumour cells. So, the VEGF-NPs offer a promising active targeting carrier for tumour selective treatment.