Resveratrol loaded zein nanoparticles (Res ZNPs) were synthesized to deliver resveratrol to bone cells for inhibiting the proliferation of osteosarcoma cells. Zein chemically cross-linked with alendronate as a bone-targeting agent using EDC and NHS chemistry was also synthesized and the cross-linking was confirmed using Fourier-Transform Infrared and Nuclear Magnetic Resonance spectroscopy. Subsequently, Res ZNPs with and without alendronate were synthesized and characterized. The particles measured 273 to 294 nm with a narrow polydispersity index, and a zeta potential of -29 to -33 mV, respectively as evaluated by dynamic light scattering. The particles showed spherical morphology imaged by transmission electron microscopy and the entrapment efficiency and loading capacity were 63.0 % and 13.6 % for Res ZNPs and 69.1 % and 21.0 % for Res ZNPs with alendronate, respectively. Furthermore, the entrapped resveratrol of both systems was released in a three-phase manner under physiological condition (phosphate-buffered saline, PBS) at 37 °C over 24 h. Both systems exhibited suppression of osteosarcoma MG-63 cell proliferation and the inhibition rate was found slightly higher for targeted, Res ZNPs with alendronate. This research suggested that Res ZNPs conjugated with alendronate could be a candidate for effective bone-targeting delivery systems to inhibit the proliferation of osteosarcoma cells.