A tissue dose-based comparative exposure assessment of manganese using physiologically based pharmacokinetic modeling-The importance of homeostatic control for an essential metal

Toxicol Appl Pharmacol. 2017 May 1:322:27-40. doi: 10.1016/j.taap.2017.02.015. Epub 2017 Feb 22.

Abstract

A physiologically-based pharmacokinetic (PBPK) model (Schroeter et al., 2011) was applied to simulate target tissue manganese (Mn) concentrations following occupational and environmental exposures. These estimates of target tissue Mn concentrations were compared to determine margins of safety (MOS) and to evaluate the biological relevance of applying safety factors to derive acceptable Mn air concentrations. Mn blood concentrations measured in occupational studies permitted verification of the human PBPK models, increasing confidence in the resulting estimates. Mn exposure was determined based on measured ambient air Mn concentrations and dietary data in Canada and the United States (US). Incorporating dietary and inhalation exposures into the models indicated that increases in target tissue concentrations above endogenous levels only begin to occur when humans are exposed to levels of Mn in ambient air (i.e. >10μg/m3) that are far higher than those currently measured in Canada or the US. A MOS greater than three orders of magnitude was observed, indicating that current Mn air concentrations are far below concentrations that would be required to produce the target tissue Mn concentrations associated with subclinical neurological effects. This application of PBPK modeling for an essential element clearly demonstrates that the conventional application of default factors to "convert" an occupational exposure to an equivalent continuous environmental exposure, followed by the application of safety factors, is not appropriate in the case of Mn. PBPK modeling demonstrates that the relationship between ambient Mn exposures and dose-to-target tissue is not linear due to normal tissue background levels and homeostatic controls.

Keywords: MOS; Manganese; Margin of safety; PBPK; Pharmacokinetics.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Canada / epidemiology
  • Dose-Response Relationship, Drug
  • Environmental Exposure / adverse effects
  • Homeostasis / drug effects
  • Homeostasis / physiology*
  • Humans
  • Inhalation Exposure / adverse effects*
  • Manganese / adverse effects
  • Manganese / pharmacokinetics*
  • Models, Biological*
  • Nutrition Surveys / methods
  • Occupational Exposure / adverse effects
  • Particulate Matter / adverse effects
  • Particulate Matter / pharmacokinetics
  • Tissue Distribution / drug effects
  • Tissue Distribution / physiology
  • Trace Elements / adverse effects
  • Trace Elements / pharmacokinetics*
  • United States / epidemiology

Substances

  • Particulate Matter
  • Trace Elements
  • Manganese