Soy protein isolate was hydrolyzed by compound enzymes to prepare nanoparticles. Nanoparticles are spherical like and very stable in various conditions. Cellular uptake and cytotoxicity were investigated in monolayer cell model. 3-D multicellular spheroids were using to evaluate nanoparticles' effect. Antitumor effect of these nanoparticles was measured using H22 tumor-bearing mice.