Surfactant effects on the in vitro percutaneous absorption of diclofenac sodium

  • A. Arellano
  • S. Santoyo
  • C. Martn
  • P. Ygartua
Article

Summary

Nonionic surfactants, which are a safe class of enhancers, may offer means of enhancing drug permeation through the skin. In order to determine this effect, the influence of four nonionic surfactants on the percutaneous absorption of diclofenac sodium from carbopol gels containing 40% propylene glycol was investigated. In vitro diffusion experiments were carried out using excised full-thickness abdominal rat skin as well as cellulose nitrate membranes. The data of this study clearly revealed that Tween 80 decreased diclofenac penetration rate. This was due to a decrease in thermodynamic activity as a result of micellar complexation. In contrast, the more hydrophobic sorbitans enhanced diclofenac skin penetration, probably due to changes in the barrier properties of the skin and in the vehicle-stratum corneum partition coefficient. The most enhancing effect was induced by Span 20, a surfactant with a C12 saturated hydrophobic group. However, diffusional lag times for all the tested surfactants were longer than for the control gel.

Keywords

Diclofenac sodium percutaneous absorption penetration enhancer nonionic surfactant release rate 
This is a preview of subscription content, log in to check access.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Ashton P., Hadgraft J., Walters K.A. (1986): Effects of surfactants in percutaneous absorption. Pharm. Acta Helv. 61, 228–235.PubMedGoogle Scholar
  2. 2.
    Sarpotdar P.P., Zatz J.L. (1986): Evaluation of penetration enhancement of lidocaine by nonionic surfactants through hairless mouse skin in vitro. J. Pharm. Sci. 75, 176–181.CrossRefPubMedGoogle Scholar
  3. 3.
    Cappel M.J., Kreuter J. (1991): Effect of nonionic surfactants on transdermal drug delivery: I. Polysorbates. Int. J. Pharm. 69, 143–153.CrossRefGoogle Scholar
  4. 4.
    Hwang C., Danti A.G. (1983): Percutaneous absorption of flufenamic acid in rabbits: effects of dimethyl sulfoxide and various nonionic surface-active agents. J. Pharm. Sci. 72, 857–860.CrossRefPubMedGoogle Scholar
  5. 5.
    Walters K.A. (1989): Penetration enhancers and their use in transdermal therapeutic systems. In: Hadgraft, J., Guy, R.H. (Eds). Transdermal drug delivery. Marcel Dekker, Inc., New York, pp 197–246.Google Scholar
  6. 6.
    Ashton P., Walters K.A., Brain K.R., Hadgraft J. (1992): Surfactant effects in percutaneous absorption. I. Effects on transdermal flux of methyl nicotinate. Int. J. Pharm. 87, 261–264.CrossRefGoogle Scholar
  7. 7.
    Nishihata T., Kotera K., Nakano Y., Yamazaki M. (1987): Rat percutaneous transport of diclofenac and influence of hydrogenated soya phospholipids. Chem. Pharm. Bull. 35, 3807–3812.PubMedGoogle Scholar
  8. 8.
    Higuchi W.I. (1962): Analysis of data on the medicament release from ointments. J. Pharm. Sci.51, 802–804.CrossRefPubMedGoogle Scholar
  9. 9.
    Aungust B.J., Rogers N.J., Shefter E. (1986). Enhancement of naloxone penetration through human skin in vitro using fatty acids, fatty alcohols, surfactants, sulfoxides and amides. Int. J. Pharm. 33, 225–234.CrossRefGoogle Scholar
  10. 10.
    Chowhan Z.T., Pritchard R. (1978): Effect of surfactants on percutaneous absorption of naproxen. I: comparisons of rabbit, rat and human excised skin. J. Pharm. Sci. 67, 1272–1274.CrossRefPubMedGoogle Scholar
  11. 11.
    Shahi V., Zatz J.L. (1978): Effect of formulation factors on penetration of hydrocortisone through mouse skin. J. Pharm. Sci. 67, 789–792.CrossRefPubMedGoogle Scholar
  12. 12.
    Sarpotdar P.P., Zatz J.L. (1986): Percutaneous absorption enhancement by nonionic surfactants. Drug Dev. Ind. Pharm. 12, 1625–1647.CrossRefGoogle Scholar
  13. 13.
    Walters K.A., Olejnik O. (1983): Effects of nonionic surfactants on the hairless mouse skin penetration of methyl nicotinate. J. Pharm. Pharmacol. 35 Suppl., 79 P.Google Scholar
  14. 14.
    Koprda V., Bohacik L., Hadgraf J. (1995): Effect of penetration enhancers on the skin permeation of stobadine. In: Brain, K.R., James, V.J., Walters, K.A. (Eds). Abstracts of presentations at the Fourth International Prediction of Percutaneous Penetration Conference in La Grande Motte, C27. STS Publishing, Cardiff.Google Scholar
  15. 15.
    Shen W., Danti A.G., Bruscato F.N. (1976): Effect of nonionic surfactants on percutaneous absorption of salicylic acid and sodium salicylate in the presence of dimethyl sulfoxide. J. Pharm. Sci. 65, 1780–1783.CrossRefPubMedGoogle Scholar

Copyright information

© Springer-Verlag 1998

Authors and Affiliations

  • A. Arellano
    • 1
  • S. Santoyo
    • 1
  • C. Martn
    • 1
  • P. Ygartua
    • 1
  1. 1.Departamento de Farmacia y Tecnologia Farmacéutica, Facultad de FarmaciaUniversidad de NavarraPamplonaSpain

Personalised recommendations