The aim of this study was to prepare niacinamide (NA) imprinted biomaterials for treating hyperpigmentation using mungbean starch (MS), PVA, and plasticizers (glycerol (GL) and citric acid (CA)). Biomaterials and NA were characterized by FE-SEM, FT-IR, and 1H NMR. To evaluate the applicability of the NA imprinted biomaterials for a transdermal drug delivery system (TDDS), NA release experiment was conducted in different pH and temperature conditions. Results of NA release properties indicated that NA was released about 99 % rapidly in the initial 10 min. NA release in low pH and high temperature was also higher than that in high pH and low temperature. The determination of experimental conditions and the analysis of NA release results were achieved using response surface methodology (RSM). Results of NA release using artificial skin indicated that NA release from NA imprinted biomaterials was increased at a relatively steady rate for 90 min. To verify for treating hyperpigmentation of the prepared biomaterials, tyrosinase inhibitory and antioxidant inhibitory were performed. Results indicated that NA imprinted biomaterials with the addition of CA exhibited 55.8 % of tyrosinase inhibitory and 73.0 % of antioxidant inhibitory. In addition, their ability to inhibit melanin synthesis in B16F10 cells was evaluated.