DSPE-PEG1000-iRGD is a PEG compound made from DSPE and the αv-integrin-targeting peptide (iRGD). The iRGD peptide initially binds to αv-integrins and undergoes proteolytic cleavage within tumors to produce CRGDK/R, which interacts with neuropilin-1, thereby facilitating tumor targeting and penetration. DSPE-PEG1000-iRGD is useful for drug delivery applications.