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In Vitro and In Vivo Studies of Topical Delivery System of Gentisic Acid in Hairless Mice

  • Bian, Shengjie (College of Pharmacy, Pusan National University,Department of Pharmacy, Shenyang Pharmaceutical University) ;
  • Zheng, Junmin (Department of Pharmacy, Shenyang Pharmaceutical University) ;
  • Kim, Jung-Sun (Department of Biotechnology, Dongseo University) ;
  • Choi, Myeong-Jun (Charmzone Biomaterial Research Center) ;
  • Chung, Ho-Kwon (Charmzone Biomaterial Research Center) ;
  • Lee, Chi-Ho (College of Pharmacy, Pusan National University) ;
  • Kim, Dae-Duk (College of Pharmacy, Pusan National University)
  • Published : 2002.09.20

Abstract

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 DuroTak 87-2510 patch formulation permeated across hairless mouse skin at the rate of $40.79\;{\mu}g/cm^2/hr$. 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 skin-whitening agent into the epidermis/dermis layer, the target site.

Keywords

References

  1. E.V. Curto, C. Kwong, H. Hermersdorfer, H. Glatt, C. Santis, V.Virador, J.V.Hearing and T.P. Dooley, Inhibitors of mammalian melanocyte tyrosinase: in vitro comparisons of alkyl esters of gentisic acid with other putative inhibitors, Biochem. Pharmacol., 57, 663-672 (1999) https://doi.org/10.1016/S0006-2952(98)00340-2
  2. L.K. Pershing, J. Corlett and C. Jorgensen, In vivo pharma- cokinetics and pharmacodynamics of topical ketoconazole and miconazole in human stratum corneum, Agents Chemother., 38, 90-95 (1994) https://doi.org/10.1128/AAC.38.1.90
  3. L.A. Goldsmith, Physiology, Biochemistry and Molecular Biology of the Skin, Oxford University Press, Oxford, U.K., pp. 873-909 (1991)
  4. S. Bian, H. J. Doh, J. Zheng, J. S. Kim and D. D. Kim, In vitro evaluation of patch formulation for topical delivery of gentisic acid in rats. Eur. J. Pharm. Sci., submitted (2002)
  5. T.K. Ghosh and W.R. Pfister, Transdermal and Topical Drug Delivery Systems, Interpharm Press, Buffalo Grove, U.S.A., pp. 593-612 (1997)
  6. J.C. Tsai, S.A. Chuang, M.Y. Hsu and H.M. Sheu, Distribution of salicylic acid in human stratum corneum following topical application in vivo: a comparison of six different formulations, Int. J. Pharm., 188, 145-153, (1999) https://doi.org/10.1016/S0378-5173(99)00217-3
  7. L. Coderch, M. Oliva, M. Pons, A. de la Maza, A.M. Manich and J.L. Parra, Percutaneous penetration of liposomes using the tape-stripping technique, Int. J. Pharm., 139, 197-203, (1996) https://doi.org/10.1016/0378-5173(96)04620-0
  8. I. Alberti, Y.N. Kalia, A. Naik, J.D. Bonny and R.H. Guy, In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum, J. Controlled Release, 71, 319-327, (2001) https://doi.org/10.1016/S0168-3659(01)00244-9
  9. D.D. Kim and Y.W. Chien, Transdermal delivery of dideoxy- nucleoside-type anti-HIV drugs. 1. Stability studies for hairless rat skin permeation, J. Pharm. Sci. 84, 1061-6, (1995) https://doi.org/10.1002/jps.2600840906
  10. A. Rougier, D. Dupuis, C. Lotte and R., Roguet, The measurement of the stratum corneum reservoir. A predictive method for in vivo percutaneous absorption studies: influence of application time, J. Invest. Dermatol., 84, 66-68, (1985) https://doi.org/10.1111/1523-1747.ep12274834
  11. P. Morganti, The cosmetic patch: a new frontier in cosmetic dermatology, Sop Cosm. Chem. Spec., 72(2), 48-50 (1996)
  12. W. R. Pfister and V. J. Rajadhyaksha, Oxazolidinones: a new class of cyclic urethane trnasdermal enhancers. Pharm. Res., 12(9), S280 (1995)