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j. Cosmet. Sci., 54, 483-491 (September/October 2003) Penetration enhancement in mouse skin and lipolysis in adipocytes by TAT-GKH, a new cosmetic ingredient JUN MAN LIM, MIN YOUL CHANG, SUN GYOO PARK, NAE GYU KANG, YOUNG SOOK SONG, YOUNG HWA LEE, YOUNG CHANG YOO, WAN GOO CHO, SOO YOUNG CHOI, and SHE HOON KANG, Cosmetic ROD Center, LG Household O Healthcare Research Park 84, Jang-dong, Yusong-gu, Taejon 305-343 (J.M.L., M.Y.C., S.G.P., N.G.K., Y.S.S., Y.H.L., Y.C.Y., W.G.C., S.E.K.), and Division of Lij• Sciences, Hallym University, Chunchon 200-702 (S. Y.C.), Korea. Accepted for publication November 15, 2002. Synopsis Since the basic domain of human immunodeficiency virus type I (HIV-1) transactivator of transcription (TAT) protein was reported to possess the ability to traverse biological membranes efficiently, various therapeutic proteins have been attached to TAT for the purpose of therapy. In this study, the tripeptide GKH (glycine-lysine-histidine) derived from parathyroid hormone (PTH), known as lipolytic peptide, was attached to 9-poly lysine (TAT) to be used as a cosmetic ingredient in slimming products. TAT-GKH at 10 -5 M induced approximately 37.6% and 41.5% maximal lipolytic effects in cultured 3T3-L1 differen- tiated adipocytes and in epididymal adipocytes isolated from rats, respectively, compared with basal lipoly- sis. The lipolytic effect of GKH was not changed by TAT-GKH fusion. In cytotoxicity tests, there was no cytotoxicity in any dose concentration of TAT-GKH. We confirmed that TAT-GKH induced lipolytic activity by GKH without cytotoxicity and with the possibility of its use as a safe cosmetic ingredient. TAT-GKH elevated penetration into excised hairless mice skin 36 times more efficiently than GKH. TAT-GKH can be used as a cosmetic ingredient in slimming products, with both penetration enhancement and lipolytic effect without cytotoxicity. INTRODUCTION In the effort to overcome the limiting barrier of drug delivery to skin, various physical and chemical vehicles such as micelies, liposomes, microemulsions, and nanoparticles have been used in cosmetic science as well as in pharmaceutical science. However, these approaches have been observed not only to be dependent on the applied constituents of Address all correspondence to Jun Man Lim. 483