Current challenges and future perspectives in oral absorption research: An opinion of the UNGAP network

Zahari Vinarov, Bertil Abrahamsson, Per Artursson, Hannah Batchelor, Philippe Berben, Andreas Bernkop-Schnurch, James Butler, Jens Ceulemans, Nigel Davies, Didier Dupont, Goril Eide Flaten, Nikoletta Fotaki, Brendan T. Griffin, Vincent Jannin, Janneke Keemink, Filippos Kesisoglou, Mirko Koziolek, Martin Kuentz, Alan Mackie, Antonio J. Melendez-MartinezMark McAllister, Anette Mullertz, Caitriona M. O'Driscoll, Neil Parrott, Jadwiga Paszkowska, Petr Pavek, Christopher J. H. Porter, Christos Reppas, Cordula Stillhart, Kiyohiko Sugano, Elena Toader, Katerina Valentova, Maria Vertzoni, Saskia N. De Wildt, Clive G. Wilson, Patrick Augustijns*

*Corresponding author for this work

Research output: Contribution to journalReviewResearchpeer-review

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Abstract

Although oral drug delivery is the preferred administration route and has been used for centuries, modern drug discovery and development pipelines challenge conventional formulation approaches and highlight the insufficient mechanistic understanding of processes critical to oral drug absorption. This review presents the opinion of UNGAP scientists on four key themes across the oral absorption landscape: (1) specific patient populations, (2) regional differences in the gastrointestinal tract, (3) advanced formulations and (4) food-drug interactions. The differences of oral absorption in pediatric and geriatric populations, the specific issues in colonic absorption, the formulation approaches for poorly water-soluble (small molecules) and poorly permeable (peptides, RNA etc.) drugs, as well as the vast realm of food effects, are some of the topics discussed in detail. The identified controversies and gaps in the current understanding of gastrointestinal absorption-related processes are used to create a roadmap for the future of oral drug absorption research.

(c) 2021 The Author(s). Published by Elsevier B.V. This is an open access article under the CC BY license (http:// creativecommons.org/licenses/by/4.0/).

Original languageEnglish
JournalAdvanced Drug Delivery Reviews
Volume171
Pages (from-to)289-331
Number of pages43
ISSN0169-409X
DOIs
Publication statusPublished - 2021

Keywords

  • Specific patient populations
  • Regional differences
  • Advanced formulations
  • Amorphous solid dispersions
  • Lipid-based formulations
  • Food-drug interactions
  • Microbiome
  • In vitro tools
  • PBPK modeling
  • IN-VITRO MODELS
  • BIOPHARMACEUTICS TOOLS PROJECT
  • LIPID-BASED FORMULATIONS
  • DRUG-DELIVERY SYSTEMS
  • DOSAGE FORMS
  • BIORELEVANT DISSOLUTION
  • PHARMACOKINETIC PBPK
  • VIVO PERFORMANCE
  • FED STATE
  • INTESTINAL PERMEABILITY

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