This study was aimed at investigating the effects of roasting and cryogenic milling on particle size, water solubility, and amount of bioactive components in ginseng root. Samples were pulverized by cryogenic milling, and one treatment condition was selected for each size range (10-50 μm, and >50 μm). The selected samples were roasted at different temperatures (160-200 °C) followed by cryogenic milling. Powdered samples were analyzed for their physicochemical characteristics. Results revealed that roasted samples exhibited significantly smaller particle size than controls (not roasted, p<0.05), and the particle size of roasted samples decreased with increase in roasting temperature until flocculation occurred around 180-190 °C. With decrease in particle size of ginseng; water solubility index, antioxidant activity, total polyphenol content, and total polysaccharide content were observed to increase. Ginseng samples showed an increasing trend in antioxidant activity with decreasing particle size (p>0.05) with significantly higher values for all roasted samples compared to the controls (p<0.05). Non-polar ginsenosides such as Rg2(S), Rg2(R), Rg3(S), Rg3(R), and Rh1(S) showed an increase in temperature-dependent manner. This study revealed that roasting at certain temperature range with cryogenic milling has positive effects on ginseng by reducing its particle size, and increasing water solubility and bioactive components.