Membrane permeability in the gastrointestinal tract: the interplay between microclimate pH and transporters

Chemistry & Biodiversity
Albin Kristl

Abstract

Some examples of pH- and transporter-dependent permeability, determined in side-by-side diffusion cells, are summarized. We investigated the polarized transport in the mucosal-to-serosal direction of monocarboxylic acid-type drugs through the excised rat jejunal tissue and an artificial membrane. We established that, in vitro, these substances are most probably not transported by monocarboxylate transporter 1, but by passive pH-dependent transport. We also studied various influences on the permeability of fluorescein, a low permeability marker, through isolated rat intestinal segments, Caco-2 cell monolayers, and an artificial membrane. Polarized transport of fluorescein in the serosal-to-mucosal direction through the rat jejunum by multidrug resistance-associated protein was triggered by the addition of D-glucose to the mucosal side, while the pH-dependent increase of fluorescein influx is presumably the consequence of a monocarboxylate transporter and a member of the organic-anion transporting polypeptide family. With permeability experiments through the excised segments of rat small intestine, we ascertained that ciprofloxacin is a low-permeability drug and has higher and pH-dependent transport in the mucosal-to-serosal dire...Continue Reading

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Citations

Aug 21, 2010·Analytical Chemistry·Su LiNoah Malmstadt
Jan 8, 2013·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·R A RochaD Vélez
Oct 1, 2016·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Silvia PichardoAna M Cameán
Mar 14, 2011·Molecular Informatics·G Valsami, P Macheras

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