Insulin permeability across an in vitro dynamic model of endothelium

Pharm Res. 2002 Apr;19(4):445-50. doi: 10.1023/a:1015187410909.

Abstract

Purpose: Endothelium insulin permeability was investigated using in vitro, dynamic culture of endothelial cells.

Methods: Endothelial cells were cultured in a hollow fiber apparatus and continuously exposed to a flow. Transendothelial electrical resistance and permeability to [14C]sucrose and [14C]inulin were used to monitor the integrity of the endothelial monolayer.

Results: Under these experimental conditions, measurements of insulin permeability, investigated at increasing hormone concentrations, suggested that the predominant transendothelial insulin fluxes were attributable to bidirectional convective transport rather than to a saturable transport mechanism, in agreement with in vivo experiment results published earlier. Analytical determinations of insulin catabolism demonstrated a low percent of insulin degradation by the endothelium, leading to production of insulin metabolites qualitatively identical to those produced by human monocytes.

Conclusions: The findings of this paper indicated that (a) insulin crosses the endothelial monolayer by paracellular "leak" and endothelial insulin receptors have a minor (if any) role in insulin transport; (b) degradation of the hormone by BAEC is minimal; (c) the in vitro, dynamic culture of endothelial cells presented here should represent a valuable transport model system to study permeability mechanisms of insulin and many other drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cattle
  • Cell Membrane Permeability / drug effects*
  • Cells, Cultured
  • Electric Impedance
  • Endothelium, Vascular / cytology*
  • Endothelium, Vascular / metabolism*
  • In Vitro Techniques
  • Insulin / metabolism
  • Insulin / pharmacokinetics*
  • Models, Biological*

Substances

  • Insulin