Gardeniae Fructus is consisted of geniposide and its derivatives. For the purpose of treatment of skin disease, geniposide and hydrolyzed products (HP) of Gardeniae Fructus were studied on skin permeation and crosslinking with biological tissue. The hydrolyzed products (HP) and active ingredients of Gardeniae Fructus were identified and investigated about skin permeability. Genipin has provided low cytotoxic crosslinking reagents and formed stable and biocompatible crosslinked products. The permeation enhancing effects of geniposide and genipin under the hydrolyzed products of cream and hydrogel preparations were tested using Franz type diffusion cell and the skin of hairless mouse. The remaining pro-portions of geniposide and genipin were measured in the hydrolyzed products of cream and hydrogel preparations. The crosslinking of epidermic and endodermic tissue with genipin under the hydrolyzed prodcuts of cream and hydrogel preparation was observed using light microscopy. Increased absorption ratio of the skin of hairless mouse about genipin was higher than that of geniposide. Loads at break, tensile strengths and skin permeation rate of the hydrolyzed products (HP) of cream and hydrogel preparations were higher than the nonhydrolyzed products (NHP). The hydrolyzed products (HP) of cream and hydrogel of Gardeniae Fructus Extracts were proper preparations and crosslinking agents to increase the trans-dermal absorption with epidermic and endodermic tissue.