Publications
Browse peer-reviewed literature, posters, webinars, blog articles, and more showing how we and others are using RepliGut Systems to support discovery.
2021
Lemmens, Glenn; Camp, Arno Van; Kourula, Stephanie; Vanuytsel, Tim; Augustijns, Patrick
Drug Disposition in the Lower Gastrointestinal Tract: Targeting and Monitoring Journal Article
In: Pharmaceutics, vol. 13, no. 2, pp. 161, 2021, ISSN: 1999-4923, (Number: 2 Publisher: Multidisciplinary Digital Publishing Institute).
Abstract | Links | BibTeX | Tags: colon drug delivery, colonic drug disposition, colonic physiology, drug absorption, drug metabolising enzymes ({DME}), intestinal in vitro models, microbiome, microphysiological systems ({MPS})
@article{lemmens_drug_2021,
title = {Drug Disposition in the Lower Gastrointestinal Tract: Targeting and Monitoring},
author = {Glenn Lemmens and Arno Van Camp and Stephanie Kourula and Tim Vanuytsel and Patrick Augustijns},
url = {https://www.mdpi.com/1999-4923/13/2/161},
doi = {10.3390/pharmaceutics13020161},
issn = {1999-4923},
year = {2021},
date = {2021-01-26},
urldate = {2021-01-26},
journal = {Pharmaceutics},
volume = {13},
number = {2},
pages = {161},
abstract = {The increasing prevalence of colonic diseases calls for a better understanding of the various colonic drug absorption barriers of colon-targeted formulations, and for reliable in vitro tools that accurately predict local drug disposition. In vivo relevant incubation conditions have been shown to better capture the composition of the limited colonic fluid and have resulted in relevant degradation and dissolution kinetics of drugs and formulations. Furthermore, drug hurdles such as efflux transporters and metabolising enzymes, and the presence of mucus and microbiome are slowly integrated into drug stability- and permeation assays. Traditionally, the well characterized Caco-2 cell line and the Ussing chamber technique are used to assess the absorption characteristics of small drug molecules. Recently, various stem cell-derived intestinal systems have emerged, closely mimicking epithelial physiology. Models that can assess microbiome-mediated drug metabolism or enable coculturing of gut microbiome with epithelial cells are also increasingly explored. Here we provide a comprehensive overview of the colonic physiology in relation to drug absorption, and review colon-targeting formulation strategies and in vitro tools to characterize colonic drug disposition.},
note = {Number: 2
Publisher: Multidisciplinary Digital Publishing Institute},
keywords = {colon drug delivery, colonic drug disposition, colonic physiology, drug absorption, drug metabolising enzymes ({DME}), intestinal in vitro models, microbiome, microphysiological systems ({MPS})},
pubstate = {published},
tppubtype = {article}
}
The increasing prevalence of colonic diseases calls for a better understanding of the various colonic drug absorption barriers of colon-targeted formulations, and for reliable in vitro tools that accurately predict local drug disposition. In vivo relevant incubation conditions have been shown to better capture the composition of the limited colonic fluid and have resulted in relevant degradation and dissolution kinetics of drugs and formulations. Furthermore, drug hurdles such as efflux transporters and metabolising enzymes, and the presence of mucus and microbiome are slowly integrated into drug stability- and permeation assays. Traditionally, the well characterized Caco-2 cell line and the Ussing chamber technique are used to assess the absorption characteristics of small drug molecules. Recently, various stem cell-derived intestinal systems have emerged, closely mimicking epithelial physiology. Models that can assess microbiome-mediated drug metabolism or enable coculturing of gut microbiome with epithelial cells are also increasingly explored. Here we provide a comprehensive overview of the colonic physiology in relation to drug absorption, and review colon-targeting formulation strategies and in vitro tools to characterize colonic drug disposition.