Secretory transport of methylprednisolone possibly mediated by P-glycoprotein in Caco-2 cells

Biological & Pharmaceutical Bulletin
Ayako OkaB J Aungst

Abstract

We recently reported that P-glycoprotein (MDR1) is capable of interfering with the absorption of methylprednisolone in the rat small intestine. This study was undertaken to examine the interaction between methylprednisolone and MDR1 using Caco-2 cells. The permeation of various steroid hormones (hydrocortisone, prednisolone, progesterone, beta-estradiol, and testosterone) was compared. The basolateral-to-apical (secretory) permeation of methylprednisolone was more than 3-fold greater than the apical-to-basolateral (absorptive) permeation. When verapamil (0.1 mm), a potent modulator of MDR1, was added to both apical and basolateral sides of Caco-2 cells, the absorptive permeation of methylprednisolone was increased and its secretory permeation was decreased. As a result, the secretory-oriented manner of methylprednisolone permeation almost completely disappeared. Prednisolone and hydrocortisone exhibited weaker secretory-oriented movement than did methylprednisolone. The secretory-oriented permeation of prednisolone and hydrocortisone was also diminished by the addition of verapamil. There was no significant directionality in progesterone permeation and the permeation of beta-estradiol and testosterone tended to be absorptive. T...Continue Reading

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Citations

Oct 7, 2004·Biological & Pharmaceutical Bulletin·Michiya KobayashiSansei Nishibe
Apr 3, 2012·Toxicology and Applied Pharmacology·Andrew Crowe, Ai May Tan
Oct 16, 2004·The Journal of Pharmacy and Pharmacology·Hiroki KonishiAkira Yamaji
Dec 8, 2009·Clinical Immunology : the Official Journal of the Clinical Immunology Society·Ilenia DrigoGiuliana Decorti
Feb 7, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Hiroshi SaitohBruce J Aungst
Apr 19, 2015·International Journal of Pharmaceutics·Ye ShengAshim K Mitra
Jul 14, 2010·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Paulo PaixãoJosé A G Morais
Jun 17, 2016·Expert Opinion on Drug Metabolism & Toxicology·Fernando de AndrésPaolo Martelletti
Nov 9, 2007·Pharmaceutical Research·Ching-Lin ChenJiahorng Liaw
Jun 3, 2004·Nature Reviews. Drug Discovery·Diane E MilenicMartin W Brechbiel
Feb 18, 2017·Clinical Pharmacokinetics·Anton IvanyukThierry Buclin

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