Archives of Dermatological Research

, Volume 309, Issue 6, pp 423–431

Skin permeation and antioxidant efficacy of topically applied resveratrol

  • Cristina Alonso
  • M. Martí
  • C. Barba
  • V. Carrer
  • L. Rubio
  • L. Coderch
Original Paper
  • 191 Downloads

Abstract

The permeation of resveratrol was assessed by in vitro and in vivo experiments 24 h after topical administration. The in vitro profile of resveratrol was assessed by Raman spectroscopy. Human skin permeation was analysed in vivo by the tape stripping method with the progressive removal of the stratum corneum layers using adhesive tape strips. Moreover, the free radical scavenging activity of resveratrol after its topical application was determined using the DPPH assay. The Raman spectra indicated that the topically applied resveratrol penetrates deep into the skin. The results showed high amounts of resveratrol in the different stratum corneum layers close to the surface and a constant lower amount in the upper layers of the viable epidermis. The concentration of resveratrol present in the outermost stratum corneum layers was obtained by tape stripping after in vivo application. The results demonstrated that resveratrol mainly remained in the human stratum corneum layers. After topical application, resveratrol maintained its antiradical activity. The antioxidant efficacy of the compound was higher in the inner layers of the stratum corneum. As these results have demonstrated, topically applied resveratrol reinforces the antioxidant system of the stratum corneum and provides an efficient means of increasing the tissue levels of antioxidants in the human epidermis.

Keywords

Resveratrol Percutaneous absorption In vivo In vitro Antiradical activity 

References

  1. 1.
    Acquaviva R, Russo A, Campisi A, Sorrenti V, Di Giacomo C, Barcellona ML, Avitabile M, Vanella A (2002) Antioxidant activity and protective effect on DNA cleavage of resveratrol. J Food Sci 67:137–141. doi:10.1111/j.1365-2621.2002.tb11373.x CrossRefGoogle Scholar
  2. 2.
    Alonso C, Ramon E, Lozano C, Parra JL, Torres JL, Coderch L (2004) Percutaneous absorption of flavan-3-ol conjugates from plant procyanidins. Drug Exp Clin Res 30:1–10Google Scholar
  3. 3.
    Alonso C, Rubio L, Touriño S, Martí M, Barba C, Fernández-Campos F, Coderch L, Luís Parra J (2014) Antioxidative effects and percutaneous absorption of five polyphenols. Free Radical Biol Med 75:149–155. doi:10.1016/j.freeradbiomed.2014.07.014 CrossRefGoogle Scholar
  4. 4.
    Amr S, Brown MB, Martin GP, Forbes B (2001) Activation of clindamycin phosphate by human skin. J Appl Microbiol 90:550–554. doi:10.1046/j.1365-2672.2001.01282.x CrossRefPubMedGoogle Scholar
  5. 5.
    Baur JA, Sinclair DA (2006) Therapeutic potential of resveratrol: the in vivo evidence. Nat Rev Drug Discov 5:493–506. doi:10.1038/nrd2060 CrossRefPubMedGoogle Scholar
  6. 6.
    Bhat KP, Pezzuto JM (2002) Cancer chemopreventive activity of resveratrol. Ann NY Acad Sci 957:210–229. doi:10.1111/j.1749-6632.2002.tb02918.x CrossRefPubMedGoogle Scholar
  7. 7.
    Bradamante S, Barenghi L, Villa A (2004) Cardiovascular protective effects of resveratrol. Cardiovasc Drug Rev 22:169–188. doi:10.1111/j.1527-3466.2004.tb00139.x CrossRefPubMedGoogle Scholar
  8. 8.
    Bronaugh RL, Stewart RF, Congdon ER (1982) Methods for in vitro percutaneous absorption studies. II. Animal models for human skin. Toxicol Appl Pharm 62:481–488. doi:10.1016/0041-008X(82)90149-1 CrossRefGoogle Scholar
  9. 9.
    Caspers PJ, Lucassen GW, Carter EA, Bruining HA, Puppels GJ (2001) In vivo confocal Raman microspectroscopy of the skin: noninvasive determination of molecular concentration profiles. J Invest Dermatol 116:434–442. doi:10.1046/j.1523-1747.2001.01258.x CrossRefPubMedGoogle Scholar
  10. 10.
    Chandrasekar D, Madhusudhana K, Ramakrishna S, Diwan PV (2006) Determination of DPPH free radical scavenging activity by reversed-phase HPLC: a sensitive screening method for polyherbal formulations. J Pharm Biomed Anal 40:460–464. doi:10.1016/j.jpba.2005.07.042 CrossRefPubMedGoogle Scholar
  11. 11.
    Deostri JE (2000) Antioxidant polyphenols in tea, cocoa and wine. Nutrition 16:692–694. doi:10.1016/S0899-9007(00)00304-X CrossRefGoogle Scholar
  12. 12.
    Fauconneau B, Waffo-Teguo P, Huguet F, Barrier L, Decendit A, Merillon JM (1997) Comparative study of radical scavenger and antioxidant properties of phenolic compounds from Vitis vinifera cell cultures using in vitro tests. Life Sci 61:2103–2110. doi:10.1016/S0024-3205(97)00883-7 CrossRefPubMedGoogle Scholar
  13. 13.
    Fernandez C, Nielloud F, Fortune R, Vian L, Marti-Mestres G (2002) Benzophenone-3: rapid prediction and evaluation using non-invasive methods of in vivo human penetration. J Pharm Biomed Anal 28:57–63. doi:10.1016/S0731-7085(01)00630-6 CrossRefPubMedGoogle Scholar
  14. 14.
    Fitzpatrick TB, Eisen AZ, Wolff K, Freedberg IM (1993) Dermatology in general medicine. McGraw-Hill, New YorkGoogle Scholar
  15. 15.
    Frémont L (2000) Biological effects of resveratrol. Life Sci 66:663–673. doi:10.1016/S0024-3205(99)00410-5 CrossRefPubMedGoogle Scholar
  16. 16.
    Hung CF, Lin YK, Huang ZR, Fang JY (2008) Delivery of resveratrol, a red wine polyphenol, from solutions and hydrogels via the skin. Biol Pharm Bull 31:955–962. doi:10.1248/bpb.31.955 CrossRefPubMedGoogle Scholar
  17. 17.
    Iacopini P, Baldi M, Storchi P, Sebastiani L (2008) Catechin, epicatechin, quercetin, rutin and resveratrol in red grape: content, in vitro antioxidant activity and interactions. J Food Compos Anal 21:589–598. doi:10.1016/j.jfca.2008.03.011 CrossRefGoogle Scholar
  18. 18.
    Jang M, Cai L, Udeani GO, Slowing KV, Thomas CF, Beecher CWW, Fong HHS, Farnsworth NR, Kinghorn AD, Mehta RG, Moon RC, Pezzuto JM (1997) Cancer chemopreventive activity of resveratrol, a natural product derived from grapes. Science 275:218–220. doi:10.1126/science.275.5297.218 CrossRefPubMedGoogle Scholar
  19. 19.
    King RE, Bomser JA, Min DB (2006) Bioactivity of resveratrol. Compr Rev Food Sci Food Saf 5:65–70. doi:10.1111/j.1541-4337.2006.00001.x CrossRefGoogle Scholar
  20. 20.
    Lademann J, Jacobi U, Surber C, Weigmann HJ, Fluhr JW (2009) The tape stripping procedure—evaluation of some critical parameters. Eur J Pharm Biopharm 72:317–323. doi:10.1016/j.ejpb.2008.08.008 CrossRefPubMedGoogle Scholar
  21. 21.
    Li ZD, Ma QY, Wang CA (2006) Effect of resveratrol on pancreatic oxygen free radicals in rats with severe acute pancreatitis. World J Gastroenterol 12:137–140. doi:10.3748/WJG.v12.i1.137 CrossRefPubMedPubMedCentralGoogle Scholar
  22. 22.
    Löffler H, Dreher F, Maibach HI (2004) Stratum corneum adhesive tape stripping: influence of anatomical site, application pressure, duration and removal. Brit J Dermatol 151:746–752. doi:10.1111/j.1365-2133.2004.06084.x CrossRefGoogle Scholar
  23. 23.
    Niki E (2010) Assessment of antioxidant capacity in vitro and in vivo. Free Radic Biol Med 49:503–515. doi:10.1016/j.freeradbiomed.2010.04.016 CrossRefPubMedGoogle Scholar
  24. 24.
    OECD No. 28 (2004) Guidance document for the conduct of skin absorption studies. OECD Series on Testing and Assessment No. 28. OECD Publishing, ParisCrossRefGoogle Scholar
  25. 25.
    Prusakiewicz JJ, Ackermann C, Voorman R (2006) Comparison of skin esterase activities from different species. Pharm Res 23:1517–1524. doi:10.1007/s11095-006-0273-y CrossRefPubMedGoogle Scholar
  26. 26.
    Ramon E, Alonso C, Coderch L, De la Maza A, Lopez O, Parra JL, Notario I (2005) Liposomes as alternative vehicles for sun filter formulations. Drug Deliv 12:83–88. doi:10.1080/10717540490446080 CrossRefPubMedGoogle Scholar
  27. 27.
    Redoules D, Perie J, Viode C, Mavon A, Fournier D, Daunes S, Casas C, Lougarre A, De Viguerie N (2005) Slow internal release of bioactive compounds under the effect of skin enzymes. J Invest Dermatol 125:270–277. doi:10.1111/j.0022-202X.2005.23785.x CrossRefPubMedGoogle Scholar
  28. 28.
    Rougier A, Dupuis D, Lotte C, Rouguet R, Shaefer H (1983) In vivo correlation between stratum corneum reservoir function and percutaneous absorption. J Invest Derrmatol 81:275–278. doi:10.1111/1523-1747.ep12518298 CrossRefGoogle Scholar
  29. 29.
    Rougier A, Lotte C, Maibach HI (1987) In vivo percutaneous penetration of some organic compounds related to anatomic site in humans: predictive assessment by the stripping method. J Pharm Sci 76:451–454. doi:10.1002/jps.2600760608 CrossRefPubMedGoogle Scholar
  30. 30.
    Sánchez- Moreno C, Larrauri JA, Saura-Calixto F (1998) A procedure to measure the antiradical efficiency of polyphenols. J Sci Food Agric 76:270–276. doi:10.1002/(SICI)1097-0010(199802)76:2<270:AID-JSFA945>3.0.CO;2-9 CrossRefGoogle Scholar
  31. 31.
    Schwindt DA, Wilhelm KP, Maibach HI (1998) Water diffusion characteristics of human stratum corneum at different anatomical sites in vivo. J Invest Dermatol 111:385–389. doi:10.1046/j.1523-1747.1998.00321.x CrossRefPubMedGoogle Scholar
  32. 32.
    Sengottuvelan M, Viswanathan P, Nalini N (2006) Chemopreventive effect of trans-resveratrol—a phytoalexin against colonic aberrant crypt foci and cell proliferation in 1,2-dimethylhydrazine induced colon carcinogenesis. Carcinogenesis 27:1038–1046. doi:10.1093/carcin/bgi286 CrossRefPubMedGoogle Scholar
  33. 33.
    Shah VP, Flynn GL, Yacobi A, Maibach HI, Bon C, Fleischer NM, Franz TJ, Kaplan SA, Kawamoto J, Lesko LJ, Marty JP, Pershing LK, Schaefer H, Sequeira JA, Shrivastava SP, Wilkin J, Williams RL (1998) Bioequivalence of topical dermatological dosage forms—methods of evaluation of bioequivalence. Pharm Res 15:167–171CrossRefPubMedGoogle Scholar
  34. 34.
    Tfaili S, Josse G, Angiboust JF, Manfait M, Piot O (2014) Monitoring caffeine and resveratrol cutaneous permeation by confocal Raman microspectroscopy. J Biophotonics 7:676–681. doi:10.1002/jbio.201300011 CrossRefPubMedGoogle Scholar
  35. 35.
    Tfayli A, Piot O, Manfait M (2008) Confocal Raman microspectroscopy on excised human skin: uncertainties in depth profiling and mathematical correction applied to dermatological drug permeation. J Biophotonics 1:140–153. doi:10.1002/jbio.200710004 CrossRefPubMedGoogle Scholar
  36. 36.
    Thiele JJ, Dreher F, Packer L (2000) Antioxidant defense systems in skin. In: Elsner P, Maibach H (eds) Drugs vs. cosmetics: cosmeceutical?. Dekker, New York, pp 145–187Google Scholar
  37. 37.
    Ting WW, Vest CD, Sontheimer R (2003) Practical and experimental consideration of sun protection in dermatology. Int J Dermatol 42:505–513. doi:10.1046/j.1365-4362.2003.01867.x CrossRefPubMedGoogle Scholar
  38. 38.
    Wagner H, Kostka KH, Lehr CM, Schaefer UF (2001) Interrelation of permeation and penetration parameters obtained from in vitro experiments with human skin and skin equivalents. J Control Release 75:283–295. doi:10.1016/S0168-3659(01)00396-0 CrossRefPubMedGoogle Scholar
  39. 39.
    Wiechers JW, Kelly CL, Blease TG, Dederen JC (2004) Formulating for efficacy. Int J Cosmetic Sci 26:173–182. doi:10.1111/j.1467-2494.2004.00211.x CrossRefGoogle Scholar
  40. 40.
    Ya-Xian Z, Suetake T, Tagami H (1999) Number of cell layers of the stratum corneum in normal skin—relationship to the anatomical location on the body, age, sex and physical parameters. Arch Dermatol Res 291:555–559. doi:10.1007/s004030050453 CrossRefPubMedGoogle Scholar
  41. 41.
    Zhang G, Moore DJ, Sloan KB, Flach CR, Mendelsohn R (2007) Imaging the prodrug-to-drug transformation of a 5-fluorouracil derivative in skin by confocal raman microscopy. J Invest Dermatol 127:1205–1209. doi:10.1038/sj.jid.5700690 CrossRefPubMedGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2017

Authors and Affiliations

  • Cristina Alonso
    • 1
  • M. Martí
    • 1
  • C. Barba
    • 1
  • V. Carrer
    • 1
  • L. Rubio
    • 1
  • L. Coderch
    • 1
  1. 1.Department of Chemicals and Surfactants TechnologyAdvanced Chemical Institute of Catalonia (IQAC-CSIC)BarcelonaSpain

Personalised recommendations