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In Vitro and In Vivo Studies of Topical Delivery System of Gentisic Acid in Hairless Mice
Bian, ShengJie,Zheng, JunMin,Kim, Jung-Sun,Choi, Myeong Jun,Chung, Ho-Kwon,Lee, Chi-Ho,Kim, Dae-Duk 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.3
Gentisic acid is a skin-whitening agent which inhibits the tyrosinase activity, an essential enzyme in the process of biological synthesis of melanin. Since melanin is synthesized in melanocytes located between the viable epidermis and dermis layer, drug amount delivered into the epidermis/dermis layer can provide valuable information for the biological effect of skin-whitening agents. The purpose of this study was to prepare the gentisic acid patches with 2% dodecylamine as enhancer, and to observe the in vitro skin permeation and in vivo skin deposition of gentisic acid. Gentisic acid in Duro-Tak 87-2510 patch formulation permeated across hairless mouse skin at the rate of 40.79㎍/㎠/hr. In vivo study showed that the gentisic acid amount in both the stratum corneum and the viable epidermis/dermis increased with the increase of application time. The amount of gentisic acid in the stratum corneum was higher than that in the epidermis/dermis layer, and was expected to provide a reservoir effect even after removing the patches. Thus, the patch formulation seems to be useful for the topical delivery of ski-whitening agent into the epidermis/dermis layer, the target site.