Influence of exposure dose, complex mixture, and ultraviolet radiation on skin absorption and bioactivation of polycyclic aromatic hydrocarbons ex vivo

Arch Toxicol. 2019 Aug;93(8):2165-2184. doi: 10.1007/s00204-019-02504-8. Epub 2019 Jul 8.

Abstract

Combined exposure to complex mixtures of polycyclic aromatic hydrocarbons (PAHs) and ultraviolet radiation (UVR) is suspected to enhance PAH skin permeability and skin cancer risk depending on PAH bioactivation. The impact of PAH mixtures (exposure dose, composition, and complexity) and UVR was assessed for PAH cutaneous absorption and metabolism using realistic exposure conditions and human skin explants. PAH complex mixtures were extracted from the industrial products coal tar pitch (CTP-I) and petroleum coke (PC-I). The synthetic mixture (CTP-S) was identically reconstituted using PAH standards. The applied dose was adjusted to 1 (PC-I, CTP-I) or 10 nmol (CTP-I, CTP-S) of benzo[a]pyrene (B[a]P). Unmetabolized PAHs were recovered from the skin surface, skin and medium, and then quantified by HPLC-fluorescence detection. PAH metabolites were collected from the medium and analyzed by GC-MS/MS. B[a]P and PAH penetration was lower for the highest B[a]P dose, industrial mixtures, and CTP-I compared to PC-I. Skin irradiation increased PAH penetration only for CTP-I. PAH uptake was poorly influenced by the different experimental conditions. PAH metabolism markedly decreased in the application of mixtures, leading to unmetabolized PAH accumulation in human skin. PAH metabolism was similar between CTP-I and PC-I, but was lower for the highest dose and the industrial mixtures, suggesting a saturation of xenobiotic metabolizing enzymes, as confirmed in a time-course study. UVR strongly inhibited all PAH metabolism. Altogether, these results underline the necessity to consider the reality of human exposure (PAH complex mixtures and UVR) during in vitro experiments to properly estimate skin absorption and metabolism.

Keywords: Biotransformation; Mixtures; Polycyclic aromatic hydrocarbons; Skin absorption; Toxicological interactions; Ultraviolet radiation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzo(a)pyrene / administration & dosage
  • Benzo(a)pyrene / pharmacokinetics
  • Complex Mixtures
  • Dose-Response Relationship, Drug
  • Environmental Exposure / adverse effects
  • Gas Chromatography-Mass Spectrometry
  • Humans
  • Polycyclic Aromatic Hydrocarbons / administration & dosage*
  • Polycyclic Aromatic Hydrocarbons / chemistry
  • Polycyclic Aromatic Hydrocarbons / pharmacokinetics*
  • Skin Absorption / drug effects*
  • Skin Absorption / radiation effects*
  • Tandem Mass Spectrometry
  • Ultraviolet Rays

Substances

  • Complex Mixtures
  • Polycyclic Aromatic Hydrocarbons
  • Benzo(a)pyrene