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Fluorescein transport properties across artificial lipid membranes, Caco-2 cell monolayers and rat jejunum.
Eur J Pharm Biopharm. 2007 May; 66(2):281-5.EJ

Abstract

Membrane transport characteristics of a paracellular permeability marker fluorescein were evaluated using artificial membrane, Caco-2 cell monolayers and rat jejunum, all mounted in side-by-side diffusion cells. Modified Ringer buffers with varied pH values were applied as incubation salines on both sides of artificial membrane, cell culture monolayers or rat jejunum. Passive transport according to pH partition theory was determined using all three permeability models. In addition to that, active transport of fluorescein in the M-S (mucosal-to-serosal) direction through rat jejunum was observed. The highest M-S P(app) values regarding the active transport through the rat jejunum were observed in incubation saline with pH 6.5. Fluorescein transport through the rat jejunum was inhibited by DIDS (4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid) and alpha-CHC (alpha-cyano-4-hydroxycinnamic acid). Thus, we assume that two pH-dependent influx transporters could be involved in the fluorescein membrane transport through the intestinal (jejunal) epithelium. One is very likely an MCT (monocarboxylic acid cotransporter) isoform, inhibited by specific MCT inhibitor alpha-CHC, while the involvement of the second one with overlapping substrate/inhibitor specificities (most probably a member of the organic anion-transporting polypeptide family, inhibited at least partially by DIDS) could not be excluded.

Authors+Show Affiliations

Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia. katja.sturm@ffa.uni-lj.siNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17129714

Citation

Berginc, Katja, et al. "Fluorescein Transport Properties Across Artificial Lipid Membranes, Caco-2 Cell Monolayers and Rat Jejunum." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 66, no. 2, 2007, pp. 281-5.
Berginc K, Zakelj S, Levstik L, et al. Fluorescein transport properties across artificial lipid membranes, Caco-2 cell monolayers and rat jejunum. Eur J Pharm Biopharm. 2007;66(2):281-5.
Berginc, K., Zakelj, S., Levstik, L., Ursic, D., & Kristl, A. (2007). Fluorescein transport properties across artificial lipid membranes, Caco-2 cell monolayers and rat jejunum. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 66(2), 281-5.
Berginc K, et al. Fluorescein Transport Properties Across Artificial Lipid Membranes, Caco-2 Cell Monolayers and Rat Jejunum. Eur J Pharm Biopharm. 2007;66(2):281-5. PubMed PMID: 17129714.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fluorescein transport properties across artificial lipid membranes, Caco-2 cell monolayers and rat jejunum. AU - Berginc,Katja, AU - Zakelj,Simon, AU - Levstik,Lea, AU - Ursic,Darko, AU - Kristl,Albin, Y1 - 2006/11/28/ PY - 2006/06/05/received PY - 2006/10/16/revised PY - 2006/10/30/accepted PY - 2006/11/30/pubmed PY - 2008/1/26/medline PY - 2006/11/30/entrez SP - 281 EP - 5 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 66 IS - 2 N2 - Membrane transport characteristics of a paracellular permeability marker fluorescein were evaluated using artificial membrane, Caco-2 cell monolayers and rat jejunum, all mounted in side-by-side diffusion cells. Modified Ringer buffers with varied pH values were applied as incubation salines on both sides of artificial membrane, cell culture monolayers or rat jejunum. Passive transport according to pH partition theory was determined using all three permeability models. In addition to that, active transport of fluorescein in the M-S (mucosal-to-serosal) direction through rat jejunum was observed. The highest M-S P(app) values regarding the active transport through the rat jejunum were observed in incubation saline with pH 6.5. Fluorescein transport through the rat jejunum was inhibited by DIDS (4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid) and alpha-CHC (alpha-cyano-4-hydroxycinnamic acid). Thus, we assume that two pH-dependent influx transporters could be involved in the fluorescein membrane transport through the intestinal (jejunal) epithelium. One is very likely an MCT (monocarboxylic acid cotransporter) isoform, inhibited by specific MCT inhibitor alpha-CHC, while the involvement of the second one with overlapping substrate/inhibitor specificities (most probably a member of the organic anion-transporting polypeptide family, inhibited at least partially by DIDS) could not be excluded. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/17129714/Fluorescein_transport_properties_across_artificial_lipid_membranes_Caco_2_cell_monolayers_and_rat_jejunum_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(06)00293-1 DB - PRIME DP - Unbound Medicine ER -