This invention relates to a skin prodrug composition with bisubstituted benzene bonded with two protecting groups, comprising a composition derived from 1, 4-bis (tetrahydro-2H-pyran-2-yloxy) benzene structure. Accordingly, two protecting groups can be used to increase the active time and efficacy of the skin prodrug composition to targets such as melanocyte or tyrosinase, which can facilitate the distribution of the skin prodrug composition in hypodermis to allow absorption of melanocyte or transportation and metabolism of tyrosinase.