With tumor-specific ligand-transferrin (Tf) as target, CS-INOPs containing antitumor drug doxorubicin (DOX) for cancer cell killing and fluorescent dye Rhodamine B isothiocyanate (RBITC) for simultaneously intracellular fluorescent showed improved cell uptake and cell killing through a concurrence of cell apoptosis and autophagy in the treated tumor U251 cells. Here, TF is linked to cancer.