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Enhanced In Vitro Skin Deposition Properties of Retinyl Palmitate through Its Stabilization by Pectin

  • Suh, Dong-Churl (College of Pharmacy, Chung-Ang University) ;
  • Kim, Yeongseok (College of Pharmacy, Chung-Ang University) ;
  • Kim, Hyeongmin (College of Pharmacy, Chung-Ang University) ;
  • Ro, Jieun (College of Pharmacy, Chung-Ang University) ;
  • Cho, Seong-Wan (Department of Pharmaceutics and Biotechnology, Medical Engineering College, Konyang University) ;
  • Yun, Gyiae (Department of Food Science and Technology, Chung-Ang University) ;
  • Choi, Sung-Up (Department of Food Science and Biotechnology, Dongnam Health College) ;
  • Lee, Jaehwi (College of Pharmacy, Chung-Ang University)
  • Received : 2013.11.06
  • Accepted : 2013.12.24
  • Published : 2014.01.31

Abstract

The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin demonstrated significantly increased RP distributions in the epidermis. Furthermore, it was found that skin distribution of RP could be further improved by combined use of pectin and ascorbyl palmitate (AP), due largely to their anti-oxidative effect. These results clearly demonstrate that the skin deposition properties of RP can be improved by stabilizing RP with pectin. Therefore, it is strongly suggested that pectin could be used in the pharmaceutical and cosmetic formulations as an efficient stabilizing agent and as skin penetration modulator.

Keywords

References

  1. Antille, C., Tran, C., Sorg, O. and Saurat, J. H. (2004) Penetration and metabolism of topical retinoids in ex vivo organ-cultured full-thickness human skin explants. Skin Pharmacol. Physiol. 17, 124-128. https://doi.org/10.1159/000077238
  2. Boehnlein, J., Sakr, A., Lichtin, J. L. and Bronaugh, R. L. (1994) Characterization of esterase and alcohol dehydrogenase activity in skin. Metabolism of retinyl palmitate to retinol (vitamin A) during percutaneous absorption. Pharm. Res. 11, 1155-1159. https://doi.org/10.1023/A:1018941016563
  3. Carlotti, M. E., Rossatto, V. and Gallarate, M. (2002) Vitamin A and vitamin A palmitate stability over time and under UVA and UVB radiation. Int. J. Pharm. 20, 85-94.
  4. Carlotti, M. E., Rossatto, V., Gallarate, M., Trotta, M. and Debernardi, F. (2004) Vitamin A palmitate photostability and stability over time. J. Cosmet. Sci. 55, 233-252.
  5. Carlotti, M. E., Sapino, S., Trotta, M., Battaglia, L., Vione, D. and Pelizzetti, E. (2005) Photostability and stability over time of retinyl palmitate in an O/W emulsion and in SLN introduced in the emulsion. J. Disper. Sci. Technol. 26, 125-138. https://doi.org/10.1081/DIS-200045403
  6. Cort, W. M. (1974) Antioxidant activity of tocopherols, ascorbyl palmitate, and ascorbic acid and their mode of action. J. Am. Oil. Chem. Soc. 51, 321-325. https://doi.org/10.1007/BF02633006
  7. Harrison, J. E., Watkinson, A. C., Green, D. M., Hadgraft, J. and Brain, K. (1996) The relative effect of Azone and Transcutol on permeant diffusivity and solubility in human stratum corneum. Pharm. Res. 13, 542-546. https://doi.org/10.1023/A:1016037803128
  8. Higuchi, T. (1960) Physical chemical analysis of percutaneous absorption process from creams and ointments. J. Soc. Cosmet. Chem. 11, 85-97.
  9. Hras, A. R., Hadolin, M., Knez, Z. and Bauman, D. (2000) Comparison of antioxidative and synergistic effects of rosemary extract with ${\alpha}$-tocopherol, ascorbyl palmitate and citric acid in sunflower oil. Food. Chem. 71, 229-233. https://doi.org/10.1016/S0308-8146(00)00161-8
  10. Idson, B. (1990) Vitamins in cosmetics, an update I. overview and vitamin A. Drug. Cosmet. Ind. 146, 26-91.
  11. Ihara, H., Hashizume, N., Hirase, N. and Suzue, R. (1999) Esterification makes retinol more labile to photolysis. J. Nutr. Sci. Vitaminol. 45, 353-358. https://doi.org/10.3177/jnsv.45.353
  12. Jain, A. K., Thomas, N. S. and Panchagnula, R. (2002) Transdermal drug delivery of imipramine hydrochloride. I. Effect of terpenes. J. Control. Release. 79, 93-101. https://doi.org/10.1016/S0168-3659(01)00524-7
  13. Jee, J. P., Lim, S. J., Park, J. S. and Kim, C. K. (2006) Stabilization of all-trans retinol by loading lipophilic antioxidants in solid lipid nanoparticles. Eur. J. Pharm. Biopharm. 63, 134-139. https://doi.org/10.1016/j.ejpb.2005.12.007
  14. Jenning, V., Gysler, A., Schafer-Korting, M. and Gohla, S. H. (2000) Vitamin A loaded solid lipid nanoparticles for topical use: occlusive properties and drug targeting to the upper skin. Eur. J. Pharm. Biopharm. 49, 211-218. https://doi.org/10.1016/S0939-6411(99)00075-2
  15. Kim, B. H., Lee, Y. S. and Kang, K. S. (2003) The mechanism of retinol-induced irritation and its application to anti-irritant development. Toxicol. Lett. 146, 65-73. https://doi.org/10.1016/j.toxlet.2003.09.001
  16. Moser, K., Kriwet, K., Naik, A., Kalia, Y. N. and Guy, R. H. (2001) Passive skin penetration enhancement and its quantification in vitro. Eur. J. Pharm. Biopharm. 52, 103-112. https://doi.org/10.1016/S0939-6411(01)00166-7
  17. Pena Ferreira, M. R., Costa, P. C. and Bahia, F. M. (2010) Efficacy of anti-wrinkle products in skin surface appearance: a comparative study using non-invasive methods. Skin. Res. Technol. 16, 444-449. https://doi.org/10.1111/j.1600-0846.2010.00458.x
  18. Ro, J., Kim, Y., Kim, H., Jang, S. B., Lee, H. J., Chakma, S., Jeong, J. H. and Lee, J. (2013) Anti-oxidative activity of pectin and its stabilizing effect on retinyl palmitate. Korean J. Physiol. Pharmacol. 17, 197-201. https://doi.org/10.4196/kjpp.2013.17.3.197
  19. Sane, A. and Limtrakul, J. (2009) Formation of retinyl palmitate-loaded poly(l-lactide) nanoparticles using rapid expansion of supercritical solutions into liquid solvents (RESOLV). J. Supercrit. Fluid. 51, 230-237. https://doi.org/10.1016/j.supflu.2009.09.003
  20. Scheuplein, R. J. and Blank, I. H. (1971) Permeability of the skin. Physiol. Rev. 51, 702-747. https://doi.org/10.1152/physrev.1971.51.4.702
  21. Teixeira, Z., Zanchetta, B., Melo, B. A., Oliveira, L. L., Santana, M. H., Paredes-Gamero, E. J., Justo, G. Z., Nader, H. B., Guterres, S. S. and Duran, N. (2010) Retinyl palmitate flexible polymeric nanocapsules: characterization and permeation studies. Colloids Surf. B. Biointerfaces. 81, 374-380. https://doi.org/10.1016/j.colsurfb.2010.06.016
  22. Watson, R. E., Long, S. P., Bowden, J. J., Bastrilles, J. Y., Barton, S. P. and Griffiths, C. E. (2008) Repair of photoaged dermal matrix by topical application of a cosmetic 'antiageing' product. Br. J. Dermatol. 158, 472-477.

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