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Skin Structure and Metabolism: Relevance to the Design of Cutaneous Therapeutics

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Abstract

The outer layer of the epidermis or stratum corneum is the major barrier to percutaneous absorption. It has been shown that there are numerous enzyme systems beneath the stratum corneum in the viable epidermis capable of metabolizing drugs. A number of prodrug and soft drug topical therapeutic agents have been designed. After these agents penetrate the stratum corneum, they are metabolized by the cutaneous esterase systems to the desired metabolites.

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References

  1. Voorhees, J. J., Duell, E. A., Stawiski, M. (1974) Adv. Cyclic Nucl. Res. 4, 117–162.

    Google Scholar 

  2. Aoyagi, T., Umeda, K., Iizuka, H., Miura, Y. (1981) Br. J. Dermatol. 105, 257–266.

    Google Scholar 

  3. Royer, E., Chaintreul, J., Meynadier, J., Michel, B., Guilhou, J. J., Crastes de Paulet, A. (1982) Dermatologica 165, 533–543.

    Google Scholar 

  4. Hammerstrom, S., Hamberg, M., Samuelsson, B., Duell, E., Stawiski, M., Voorhess, J. (1975) Proc. Nat. Acad. Sci. USA 72, 5130–5134.

    Google Scholar 

  5. Hammerstrom, S., Lindgras, J., Marcelo, C., Duell, E., Anderson, T., Voorhess, J. (1979) J. Invest. Dermatol. 72, 268.

    Google Scholar 

  6. Penneys, N. S., Eaglstein, W., Ziboh, V. (1980) Br. J. Dermatol. 103, 257–262.

    Google Scholar 

  7. Russel, D. H., Stawiski, M. A., Duell, E. A. (1976) Pharmacologist 18, 157.

    Google Scholar 

  8. Voorhees, J. J. (1979) Archs. Derm. 115, 943–944.

    Google Scholar 

  9. Rheinwald, J. G., Green, H. (1977) Nature 265, 421–424.

    Google Scholar 

  10. Frati, L., D'Armiento, M., Gulletta, E., Verna, R., Covelli, I. (1977) Pharm. Res. Commun. 9, 815–822.

    Google Scholar 

  11. Carpenter, G. (1979) Ann. Rev. Biochem. 48, 193–216.

    Google Scholar 

  12. Schalla, W., Schaefer, H. (1982) in: Dermal and Transdermal Absorption (Brandau, R., and B. H. Lippoid, eds.) pp. 41–72, Wissenschaftliche Verlagsgesellschaft mbH, Stuttgart, Germany.

    Google Scholar 

  13. Wester, R. C., Maibach, H. I. (1983) Drug Met. Rev. 14, 169–205.

    Google Scholar 

  14. Tauber, U. (1981) in: Dermal and Transdermal Absorption (Brandau, R., and Lippoid, B. H., eds.) pp. 134–151, Wissenschaftliche Verlagsgesellschaft mbH, Stuttgart, Germany.

    Google Scholar 

  15. Feldmann, R. J., Maibach, H. I., (1967) J. Invest. Dermatol. 48, 181–183.

    Google Scholar 

  16. Bartek, M. J., La Budde (1975) in: Animal Models in Dermatology (Maibach, H. I., ed.) pp. 103–120, Churchill Livingstone, New York.

    Google Scholar 

  17. Leung, L. C., Ando. H. Y. (1979) J. Pharm. Sci. 68, 571–574.

    Google Scholar 

  18. Smith, L. H., Holland, J. M. (1981) Toxicol. 21, 47–57.

    Google Scholar 

  19. Koa, J., Hall, J., Holland, J. M. (1982) Toxicol. Appl. Pharmacol. 68, 206–217.

    Google Scholar 

  20. Holland, J. M., Kao, J. Y., Whitaker, M. J. (1984) Toxicol. Appl. Pharmacol. 72, 272–280.

    Google Scholar 

  21. Bundgaard, H., Hoelgaard, A., Mollgaard, B. (1983) Int. J. Pharm. 15, 285–292.

    Google Scholar 

  22. Morsches, B., Holzmann, H. (1982) Arzneim.-Forsch. 32, 298–300.

    Google Scholar 

  23. Wester, R. C., Noonan, P. K., Smeach, S., Kosobud, L. (1983) J. Pharm. Sci. 72, 745–748.

    Google Scholar 

  24. Rongone, E. L. (1977) in: Advances in Modern Toxicology Vol. 4: Dermatology and Pharmacology (Marzulli, F. N., and Maibach, H. I., eds.) pp. 93–137, Hemisphere Publishing Corp., Washington D.C.

    Google Scholar 

  25. Pannatier, A., Jenner, P., Testa, B., Etter, C. (1978) Drug Met. Rev. 8, 319–343.

    Google Scholar 

  26. Noonan, P. K., Wester, R. C. (1982) in: Dermatotoxicology, second edition (Marzulli, F. N., and Maibach, H. I., eds.) pp. 71–90, Hemisphere Publishing Corp., Washington D.C.

    Google Scholar 

  27. Pohl, R., Philpot, R., Fouts, J. (1976) Drug Metab. Dispos. 4, 442–450.

    Google Scholar 

  28. Bowden, G., Slaga, T., Shapas, B., Boutwill, R. (1974) Cancer Res. 34, 2634–2642.

    Google Scholar 

  29. Cox, J. S. G., Beach, J. E., Blair, A. M. J. N., King, J., Lee, T. B., Loveday, D. E. E., Moss, G. F., Orr, T. S. C., Ritche, J. T., Sheard, P. (1970) in: Advances in Drug Research, Vol. 5 (Harper, N. J., and Simmons, A. B., eds.) pp. 115, John Wiley, New York and London.

    Google Scholar 

  30. Haider, S. A. (1977) Br. Med. J. 1, 1570–1572.

    Google Scholar 

  31. Bodor, N., Zupan, J., Selk, S. (1980) Int. J. Pharm. 7, 63–75.

    Google Scholar 

  32. Weirich, E. G., Lonfauer, J. K., Kirkwood, A. K. (1976) Dermatologica 152, 87–99.

    Google Scholar 

  33. Loftsson, T., Kaminski, J. J., Bodor, N. (1981) J. Pharm. Sci. 70, 743–749.

    Google Scholar 

  34. Loftsson, T., Kaminski, J. J., Bodor, N. (1981) J. Pharm. Sci. 70, 756–758.

    Google Scholar 

  35. Sloan, K. B., Bodor, N. (1982) J. Pharm. Sci. 12, 299–313.

    Google Scholar 

  36. Mollgaard, B., Annie, H., Bundgaard, H. (1982) J. Pharm. Sci. 71, 153–162.

    Google Scholar 

  37. Fondak, A. A., Friedman, A. E., Klein, R. J. (1975) Abstract from a symposium at Stanford University, Stanford, Calif., Aug. 26–29.

  38. Lieberman, M., Schafer, T. W., Putt, S. R. (1973) J. Invest. Dermatol. 60, 203–206.

    Google Scholar 

  39. Yu, C. D., Fox, J. L., Ho, N. F. H., Higuchi, W. I. (1979) J. Pharm. Sci. 68, 1341–1346.

    Google Scholar 

  40. Yu, C. D., Fox, J. L., Ho, N. F. H., Higuchi, W. I. (1979) J. Pharm. Sci. 68, 1347–1357.

    Google Scholar 

  41. Shannon, W. M., Baker, D. C., Higuchi, W. I. (1983) 185th National Meeting of the American Chemical Society, March 20–25, Seattle, Washington.

  42. Sloan, K. B., Hashida, M., Alexander, J., Bodor, N., Higuchi, T. (1983) J. Pharm. Sci. 72, 372–378.

    Google Scholar 

  43. Bodor, N. (1977) in: Design of Biopharmaceutical Properties by Prodrug and Analogs (Roche, E. B., ed.) pp. 98, Academy of Pharmaceutical Sciences, Washington D.C.

    Google Scholar 

  44. Kapp, J. F., Koch, H., Topert, H., Kessler, J., Gerhards, E. (1977) Arzneim.-Forsch. 27, 2191–2204.

    Google Scholar 

  45. Yeung, D., Nacht, S., Bucks, D., Maibach, H. (1982) Clin. Res. 30, 616A.

    Google Scholar 

  46. Maibach, H. I., Robertson, D. B. (1982) in: Basic and Clinical Pharmacology (Katzung, B. G., ed.) pp. 708–722, Lange Medical Publications, Calif.

    Google Scholar 

  47. Bodor, N., Kaminski, J. J., Selk, S. (1980) J. Med. Chem. 23, 469–474.

    Google Scholar 

  48. Bodor, N., Woods, R., Kaminski, J. J. (1980) J. Med. Chem. 23, 474–480.

    Google Scholar 

  49. Bodor, N., Sloan, K. B., Little, R. J., Selk, S. H., Caldwell, L. (1982) Int. J. Pharm. 10, 307–321.

    Google Scholar 

  50. Bodor, N., Sloan, K. B. (1980) U.S. Patent 4, 213, 978.

    Google Scholar 

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Authors and Affiliations

  1. Departments of Pharmacy and Pharmaceutical Chemistry, School of Pharmacy and Department of Dermatology, School of Medicine, University of California, San Francisco, CA, 94143

    Daniel A. W. Bucks

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  1. Daniel A. W. Bucks
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Bucks, D.A.W. Skin Structure and Metabolism: Relevance to the Design of Cutaneous Therapeutics. Pharm Res 1, 148–153 (1984). https://doi.org/10.1023/A:1016340423079

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