Nanodrug systems containing curcumin (Cur) encapsulated with the block copolymers poly(lactide)-d-alpha-tocopheryl poly(ethylene glycol) 1000 succinate (PLA-TPGS) and poly(lactide)-poly(ethylene glycol) (PLA-PEG) have been prepared and characterized by infrared and fluorescence spectroscopy, field-emission scanning electron microscopy (FE-SEM), and dynamic light scattering (DLS). Upon encapsulation, the highest solubility of Cur-PLA-TPGS and Cur-PLA-PGE dried powder was calculated as high as 2.40 and 2.20 mg mL(-1), respectively, an increase of about 350-fold compared to that of Cur (6.79 mu g mL(-1)). The antitumor assays (cytotoxic and antitumor-promoting assays) on Hep-G2 cellsof copolymer-encapsulated Cur nanoparticles showed the apoptotic activity due to the remarkable changes in size, morphology, and angiogenesis ability of tumor cells in all cases of the tested samples as compared with the control.