A novel dual-targeted peptide containing an alpha V integrins specific ligand anda neuropilin-1 specific motif was developed which showed an increased specifictargeting affinity to tumors. Active dual-targeted liposomes were then producedwith this peptide and exhibited greater binding activity than single-targetedliposomes in vitro. Paclitaxel entrapped in this formulation greatly increasedthe uptake of paclitaxel in the targeting cells and significantly suppressed thegrowth of HUVEC and A549 cells compared with general paclitaxel injections(Taxol) and single-targeted paclitaxel liposomes. The treatment of tumor xenograftmodels with dual-targeted paclitaxel liposomes also resulted in better tumor growthinhibition than any other treatment groups. Therefore, the dual-targeted paclitaxelliposomes prepared in the present study might be a more promising drug for cancertreatment. Furthermore, the dual-targeting approach may produce synergisticeffects that can be applied in the development of new targeted drug deliverysystems.