We co-encapsulated the chemotherapeutic agents and integrin αvβ3 inhibitor, and found that the co-encapsulation of EGFR drugs and integrin αvβ3 inhibitor by MPEG-PLA nanoparticles enables the tumor cells to uptake the EGFR drugs and integrin αvβ3 inhibitor simultaneously, which efficiently reverses the drug resistance and enhanced the cytotoxicity to tumor cells. This evidence concerns the gene EGFR and neoplasm.