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Nanotechnology-based targeting drug delivery systems have a considerable potential in medicine. Therefore, the present study aimed to designe, synthesise and characterize a nanodrug with beta lactoglobulin coating including oxali-palladium with and without folate and to compare their anti-cancer effects. The physicochemical properties of nanocapsules were studied by Dynamic light scattering (DLS), atomic force microscopy (AFM) and scanning electron microscopy (SEM). Finally, the anticancer activities of nanodrugs were investigated against human colorectal cancer cell line of HCT116 by MTT and flowcytometry methods. The results of Dynamic light scattering (DLS), scanning electron microscopy (SEM) and atomic force microscopy (AFM) showed that the average size of nanocapsules with folate were less than 40 nm. Cytotoxicity results proved the dose- and time-dependent antiproliferation and anicancer activities of nanocapsules (with folate) against HCT116. Finally, it could be concluded that folate increase anticancer activity of nanodrugs and it might be considered as a new candidate in the design and synthesis of new drugs in cancer treatment.