Quercetin in w/o microemulsion: in vitro and in vivo skin penetration and efficacy against UVB-induced skin damages evaluated in vivo

Eur J Pharm Biopharm. 2008 Aug;69(3):948-57. doi: 10.1016/j.ejpb.2008.01.012. Epub 2008 Jan 20.

Abstract

The present study evaluated the potential of a w/o microemulsion as a topical carrier system for delivery of the antioxidant quercetin. Topical and transdermal delivery of quercetin were evaluated in vitro using porcine ear skin mounted on a Franz diffusion cell and in vivo on hairless-skin mice. Skin irritation by topical application of the microemulsion containing quercetin, and the protective effect of the formulation on UVB-induced decrease of endogenous reduced glutathione levels and increase of cutaneous proteinase secretion/activity were also investigated. The w/o microemulsion increased the penetration of quercetin into the stratum corneum and epidermis plus dermis at 3, 6, 9 and 12h post-application in vitro and in vivo at 6h post-application. No transdermal delivery of quercetin occurred. By evaluating established endpoints of skin irritation (erythema formation, epidermis thickening and infiltration of inflammatory cells), the study demonstrated that the daily application of the w/o microemulsion for up to 2 days did not cause skin irritation. W/o microemulsion containing quercetin significantly prevented the UVB irradiation-induced GSH depletion and secretion/activity of metalloproteinases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / pharmacokinetics*
  • Antioxidants / pharmacology*
  • Chemistry, Pharmaceutical
  • Chromatography, High Pressure Liquid
  • Drug Carriers
  • Drug Delivery Systems
  • Electrophoresis, Polyacrylamide Gel
  • Emulsions
  • Glutathione / metabolism
  • Irritants / toxicity
  • Mice
  • Mice, Hairless
  • Oils
  • Peptide Hydrolases / chemistry
  • Peptide Hydrolases / metabolism
  • Quercetin / administration & dosage
  • Quercetin / pharmacokinetics*
  • Quercetin / pharmacology*
  • Radiation-Protective Agents / administration & dosage
  • Radiation-Protective Agents / pharmacokinetics*
  • Radiation-Protective Agents / pharmacology*
  • Skin / drug effects
  • Skin / enzymology
  • Skin Absorption
  • Ultraviolet Rays
  • Water

Substances

  • Antioxidants
  • Drug Carriers
  • Emulsions
  • Irritants
  • Oils
  • Radiation-Protective Agents
  • Water
  • Quercetin
  • Peptide Hydrolases
  • Glutathione