Vascular endothelial growth factor (VEGF) is an important target for cancer therapy. In the present study, we conjugated the novel fully-human anti-VEGF165 monoclonal antibody, mAb165, with a PEGylated liposome (lip) to produce a monoclonal antibody-conjugated PEGylated liposome (mAb-lip). Physical characterization of mAb-lips showed an average particle size of 108nm. Using a bicinchoninic acid (BCA) assay, the coupling efficiency of mAb165 conjugated to the liposome was 69.8±0.5μg mAb/μmol phospholipid. In addition, we confirmed that conjugation between mAb165 and the liposome did not affect the structure and VEGF binding affinity of the antibody. Cell uptake of mAb-lips was assessed in four cell lines: MCF-7, HepG-2, SGC-7901, and L02 cells. Confocal microscopy and flow cytometry demonstrated that there was no significant difference in cell uptake between mAb-lips and mAb-free liposome either in VEGF-expressing tumor cells or normal cells. Moreover, the cytotoxicity of paclitaxel encapsulated in mAb-lips was not increased in the four cell lines. However, in BALB/c nude mice bearing MCF-7 xenografts, mAb-lips showed superior targeting activity to tumor tissues when compared with the unmodified liposome, which was demonstrated by the fact that rhodamine-labeled mAb-lips exhibited higher fluorescence intensity in tumor tissues than the unmodified liposome. Thus, our study indicated that mAb-lips may have the potential to enhance the therapeutic index of anticancer agents through targeted delivery to tumor cells in vivo.