Repeated topical administration of all-trans-retinoic acid and plasma levels of retinoic acids in humans

J Am Acad Dermatol. 1994 Mar;30(3):428-34. doi: 10.1016/s0190-9622(94)70051-6.

Abstract

Background: Vitamin A ingestion raises plasma levels of several potentially teratogenic retinoic acids (RAs) with all-trans and 13-cis configuration, but definitive data concerning the consequences of topical administration of all-trans-RA are lacking.

Objective: The study objective was to investigate the potential for inducing systemic activity after topical administration of 0.025% all-trans-RA by measuring plasma retinoid levels.

Methods: Plasma levels of all-trans-RA, 13-cis-RA, and 4-oxo-13-cis-RA were measured in four healthy subjects before, during, and after 14 daily topical applications of all-trans-RA.

Results: Topical administration of all-trans-RA did not significantly increase plasma levels of all-trans-RA, 13-cis-RA, and 4-oxo-13-cis-RA. Significant decreases in levels of these RAs observed during the night may reflect diurnal variations of retinoid metabolism or lowered absorption of dietary vitamin A.

Conclusion: Diurnal and nutritional factors influence plasma levels of endogenous retinoids to a greater extent than topical administration of all-trans-RA at doses used for acne therapy, which on the basis of these results appears unlikely to induce systemic effects.

MeSH terms

  • Administration, Topical
  • Adult
  • Humans
  • Male
  • Tretinoin / administration & dosage*
  • Tretinoin / analogs & derivatives
  • Tretinoin / pharmacokinetics*

Substances

  • Tretinoin