In this report, we have explored the possibility to facilitate the drug delivery efficiency for cancer cells through the surface chemistry modification of gold nanoparticles (AuNPs), where the functional AuNPs were synthesized by the ligand exchange reaction between triphenyl phosphide-stabilized precursor nanoparticles and mercaptopropionic acid. Our observations demonstrate that the combination of the anticancer drug daunorubicin with relevant AuNPs could be used as an efficient way to mark the cancer cells, which may afford the potential application for the early diagnosis of the respective cancers. Besides, the synergistic enhanced effect of the relevant gold nanoparticles on the drug uptake of target cancer cells could provide a new strategy to inhibit the multidrug resistance of the respective cancers.