Gossypol chitosan (GPCS) nanoparticles have been successfully synthesized at the size of 20-40 nm through amidation process to forming base shift of polymer chains of chitosan using gossypol as a crosslinking agent. Their structure was confirmed by Fourier Transformed Infra Red (FT-IR) spectra. Morphology, stability, loading and releasing efficiency of GPCS and Cur/GPCS (Cur stands for curcumin) were thoroughly investigated by Field Emission Scanning Electron Microscopy (FESEM), FT-IR, Ultra Violet-Visible spectrophotometry (UV-Vis) and High Resolve Photoluminescence System (HRPLS). The obtained nanocarrier exhibited an excellent solubility for Cur anticancer drug as well as high stability for in vitro studies. An intensive fluorescence, allowing drug monitor/delivery, was achieved. Drug release profile was also studied. GPCS, therefore, could be considered to be a potential drug carrier for therapeutic treatment.