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Intestinal drug absorption

Bio-conjugation combined with efflux in the enterocyte determines intestinal drug absorption

The sesquiterpene lactone nobilin exhibits high membrane permeability, low relative absorption and fast bioconversion forming glucuronide, cysteine conjugate, and glutathione conjugate in the Caco-2 cell culture model.  These metabolites are transported by P-gp (the first two), apical MRP2 and basal MRP3 and possibly MRP1 out of the cell.  Inhibition of efflux resulted in diminished bioconjugation (kinetic constant kdc) and improved absorption, Fa.

  

This is an interesting interplay between phase II metabolism and carrier mediated membrane transport that can be exploited to increase intestinal drug absorption.

In this study efflux inhibitors were employed in the Caco-2 model and data evaluation was performed by kinetic multi-compartment modeling.

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Prof.
Prof. Dr. Georgios Imanidis Head of Institute for Pharma Technology Telephone : +41 61 228 56 36 E-Mail : georgios.imanidis@fhnw.ch

Institute for Pharma Technology

FHNW University of Applied Sciences and Arts Northwestern Switzerland School of Life Sciences, Institute for Pharma Technology Hofackerstrasse 30 CH - 4132 Muttenz
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