The ultimate goal of cancer therapy is to kill as many cancerous cells while minimizing damage to the normal cells nearby. However, conventional chemotherapy suffers from drug resistance and lack of selectivity and consequently increased side effects which all can be overcome by application of nanocarriers. Resveratrol (Res) is supposed to act as a chemo-preventive agent by various mechanisms but its low chemical stability and restricted bioavailability limit its therapeutic application. To afford of these limitations, Res-loaded bovine serum albumin (Res-BSA) nanocarrier was developed. Then, to elevate the cytotoxic performance of Res-BSA, chitosan (CS) was used to provide adequate positive charge on the surface of nanoparticles and consequently cause enhanced cell-uptake. The particle size of Res-BSA/CS (235 ±11 nm) showed narrow distributed nano-ranged size (PdI: 0.095) and the amount of complexed Res with NPs was found to be approximately 65% in BSA/CS complex. The successful cell uptake of Res-BSA/CS was investigated via fluorescence microscopy and flow cytometry and the results showed that Res-BSA/CS induced 1.5 times more cell internalization than Res-BSA. Consequently, cell cytotoxicity studies pointed out ~1.5 and 3 times higher cell cytotoxicity after 24 h and 48 h for Res-BSA/CS than Res in MTT assay. Thus, it can be concluded that the developed Res-loaded BSA/CS nanocarrier paves a way for efficient cancer therapy and may be considered as an attractive and promising approach to enhance the therapeutic performance of Res against cancer.