The antioxidant enzyme and DPPH radical scavenging activity with variations in drying methods of diploid and tetraploid in Platycodon grandiflorum were determined. Antioxidant enzyme activities were measured as superoxide dismutase (SOD), catalase (CAT), peroxidase (POX), and ascorbate peroxidase (APX). The roots of Platycodon grandiflorum were freeze-dried, indoor-dried, hot-air dried, and microwave dried. The root extract of P. grandiflorum have shown the highest SOD enzyme activity of 92% in tetraploid of freeze-dried and indoor-dried while diploid of microwave dried showed the lowest SOD enzyme activity of 47.5%. The activity of CAT showed higher values in the root of tetraploid than in the diploid of P. grandiflorum in all drying methods. The APX activity showed relatively higher values in the root extract of freeze-dried both the diploid and tetraploid, but the difference in comparison with other extracts was not significant. The POX activities according to drying methods of diploid and tetraploid in P. grandiflorum showed relatively high values in freeze-dried and indoor-dried compared with other drying methods, and the POX activity between the diploid and tetraploid was not significant difference in each drying method. The DPPH radical scavenging activity with variation in drying methods of diploid and tetraploid in P. grandiflorum was the highest in the freeze-dried, and was higher in tetraploid than diploid in all the concentrations. In conclusion, the root of P. grandiflorum had the potent biological activities in both diploid and tetraploid. In particular, the tetraploid root of P. grandiflorum showing high antioxidant enzyme activity could be good materials for development of source of functional healthy food.