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Membrane permeability in the gastrointestinal tract: the interplay between microclimate pH and transporters.
Chem Biodivers. 2009 Nov; 6(11):1923-32.CB

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 direction than in the opposite direction. We also established that neither the permeability of fluoroquinolones nor their solubility in different buffers was influenced by the interactions with metal cations.

Authors+Show Affiliations

Faculty of Pharmacy, University of Ljubljana, Askerceva 7, SLO-1000 Ljubljana. kristla@ffa.uni-lj.si

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19937830

Citation

Kristl, Albin. "Membrane Permeability in the Gastrointestinal Tract: the Interplay Between Microclimate pH and Transporters." Chemistry & Biodiversity, vol. 6, no. 11, 2009, pp. 1923-32.
Kristl A. Membrane permeability in the gastrointestinal tract: the interplay between microclimate pH and transporters. Chem Biodivers. 2009;6(11):1923-32.
Kristl, A. (2009). Membrane permeability in the gastrointestinal tract: the interplay between microclimate pH and transporters. Chemistry & Biodiversity, 6(11), 1923-32. https://doi.org/10.1002/cbdv.200900076
Kristl A. Membrane Permeability in the Gastrointestinal Tract: the Interplay Between Microclimate pH and Transporters. Chem Biodivers. 2009;6(11):1923-32. PubMed PMID: 19937830.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Membrane permeability in the gastrointestinal tract: the interplay between microclimate pH and transporters. A1 - Kristl,Albin, PY - 2009/11/26/entrez PY - 2009/11/26/pubmed PY - 2010/2/18/medline SP - 1923 EP - 32 JF - Chemistry & biodiversity JO - Chem Biodivers VL - 6 IS - 11 N2 - 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 direction than in the opposite direction. We also established that neither the permeability of fluoroquinolones nor their solubility in different buffers was influenced by the interactions with metal cations. SN - 1612-1880 UR - https://www.unboundmedicine.com/medline/citation/19937830/Membrane_permeability_in_the_gastrointestinal_tract:_the_interplay_between_microclimate_pH_and_transporters_ L2 - https://doi.org/10.1002/cbdv.200900076 DB - PRIME DP - Unbound Medicine ER -