Hydrolysis , Skin Permeation and In Vivo Whitening Effect of Kojic Acid Monostearate as an Antimelanogenic Agent

멜라닌생성억제제인 코직산 모노스테아레이트의 가수분해와 피부투과성 및 in vivo 미백효과

  • Ha, Yong-Ho (College of Pharamacy, Chung-Ang University) ;
  • Yu, Sung-Un (College of Pharamacy, Chung-Ang University) ;
  • Kim, Dong-Sup (Toxicology Center, Korea Food & Drug Administration) ;
  • Lim, Se-Jin (College of Pharmacy, Dongduck Women's University) ;
  • Choi, Young-Wook (Toxicology Center, Korea Food & Drug Administration)
  • 하용호 (중앙대학교 약학대학) ;
  • 유성운 (중앙대학교 약학대학) ;
  • 김동섭 (식품의약품안전본부 독성연구소) ;
  • 임세진 (동덕여자대학교 약학대학) ;
  • 최영욱 (식품의약품안전본부 독성연구소)
  • Published : 1998.02.01

Abstract

Kojic acid, antimelanogenic agent, has been widely used in cosmetics to lighten the skin color. However, it has skin irritancy and instability against pH, temperature and light. To overcome these problems and optimize the molecular structure of kojic acid (KA), a prodrug, kojic acid monostearate(KMS), has been synthesized to modify the topical drug delivery in the point of sustained release of the parent drug via enzymatic hydrolysis during skin absorption. The prodrug was tested for enzymatic hydrolysis with cytosolic fraction of hairless mouse, skin. From the in vitro skin permeation study through hairless mouse skin, we found that KMS was retained in the skin and generated KA continuously by the skin esterase cleavage. In addition, topical formulations of o/w type creams and polyolprepolymer-containing cream were further tested for whitening effects using in vivo yellow skin guinea pig model.

Keywords

References

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