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-Schnürch; James Butler; Jens Ceulemans; Nigel Davies; Didier Dupont; Gøril Eide Flaten; Nikoletta Fotaki; Brendan T Griffin; Vincent Jannin; Janneke Keemink; Filippos Kesisoglou; Mirko Koziolek; Martin Kuentz; Alan Mackie; Antonio J Meléndez Martinez; Mark McAllister; Anette Müllertz; Caitriona M O'Driscoll; Neil Parrott; Jadwiga Paszkowska; Petr Pavek; Christopher J H Porter; Christos Reppas; Cordula Stillhart; Kiyohiko Sugano; Elena Toader; Kateřina Valentová; Maria Vertzoni; Saskia De Wildt; Clive G Wilson; Patrick Augustijns

doi:10.1016/j.addr.2021.02.001

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-Schnürch, James Butler, Jens Ceulemans, Nigel Davies, Didier Dupont, Gøril Eide Flaten, Nikoletta Fotaki, Brendan T Griffin, Vincent Jannin, Janneke Keemink, Filippos Kesisoglou, Mirko Koziolek, Martin Kuentz, Alan Mackie, Antonio J Meléndez MartinezMark McAllister, Anette Müllertz, Caitriona M O'Driscoll, Neil Parrott, Jadwiga Paszkowska, Petr Pavek, Christopher J H Porter, Christos Reppas, Cordula Stillhart, Kiyohiko Sugano, Elena Toader, Kateřina Valentová, Maria Vertzoni, Saskia De Wildt, Clive G Wilson, Patrick Augustijns

Research output: Contribution to journal › Review article › peer-review

96 Citations (SciVal)

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.

Original language	English
Pages (from-to)	289-331
Number of pages	43
Journal	Advanced Drug Delivery Reviews
Volume	171
Early online date	18 Feb 2021
DOIs	https://doi.org/10.1016/j.addr.2021.02.001
Publication status	Published - 30 Apr 2021

Bibliographical note

Funding Information:
This article is based upon work from COST Action UNGAP (CA16205), supported by COST (European Cooperation in Science and Technology), funded by the Horizon 2020 Framework Programme of the European Union. The support of Dagmara Hoc, Marcela Wiater, Dorota Haznar Garbacz and Grzegorz Garbacz in the edition of a part of the article is kindly acknowledged. The work has been partially financed by Polish National Centre for Research and Development (POIR.01.02.00-00-0011/17). Supported by Ministry of Education, Youth and Sports of the Czech Republic, No. LTC19039 and LTC18003 (COST Actions UNGAP and NutRedOx) and by the Czech Science Foundation, grant number 18-00132S.

Publisher Copyright:
© 2021 The Authors

Keywords

Advanced formulations
Amorphous solid dispersions
Food-drug interactions
In vitro tools
Lipid-based formulations
Microbiome
PBPK modeling
Regional differences
Specific patient populations

ASJC Scopus subject areas

Pharmaceutical Science

Access to Document

10.1016/j.addr.2021.02.001Licence: CC BY

Cite this

Vinarov, Z., Abrahamsson, B., Artursson, P., Batchelor, H., Berben, P., Bernkop-Schnürch, A., Butler, J., Ceulemans, J., Davies, N., Dupont, D., Flaten, G. E., Fotaki, N., Griffin, B. T., Jannin, V., Keemink, J., Kesisoglou, F., Koziolek, M., Kuentz, M., Mackie, A., ... Augustijns, P. (2021). Current challenges and future perspectives in oral absorption research: An opinion of the UNGAP network. Advanced Drug Delivery Reviews, 171, 289-331. https://doi.org/10.1016/j.addr.2021.02.001

Vinarov, Z, Abrahamsson, B, Artursson, P, Batchelor, H, Berben, P, Bernkop-Schnürch, A, Butler, J, Ceulemans, J, Davies, N, Dupont, D, Flaten, GE, Fotaki, N, Griffin, BT, Jannin, V, Keemink, J, Kesisoglou, F, Koziolek, M, Kuentz, M, Mackie, A, Meléndez Martinez, AJ, McAllister, M, Müllertz, A, O'Driscoll, CM, Parrott, N, Paszkowska, J, Pavek, P, Porter, CJH, Reppas, C, Stillhart, C, Sugano, K, Toader, E, Valentová, K, Vertzoni, M, De Wildt, S, Wilson, CG & Augustijns, P 2021, 'Current challenges and future perspectives in oral absorption research: An opinion of the UNGAP network', Advanced Drug Delivery Reviews, vol. 171, pp. 289-331. https://doi.org/10.1016/j.addr.2021.02.001

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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.",

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AU - Batchelor, Hannah

AU - Berben, Philippe

AU - Bernkop-Schnürch, Andreas

AU - Butler, James

AU - Ceulemans, Jens

AU - Davies, Nigel

AU - Dupont, Didier

AU - Flaten, Gøril Eide

AU - Fotaki, Nikoletta

AU - Griffin, Brendan T

AU - Jannin, Vincent

AU - Keemink, Janneke

AU - Kesisoglou, Filippos

AU - Koziolek, Mirko

AU - Kuentz, Martin

AU - Mackie, Alan

AU - Meléndez Martinez, Antonio J

AU - McAllister, Mark

AU - Müllertz, Anette

AU - O'Driscoll, Caitriona M

AU - Parrott, Neil

AU - Paszkowska, Jadwiga

AU - Pavek, Petr

AU - Porter, Christopher J H

AU - Reppas, Christos

AU - Stillhart, Cordula

AU - Sugano, Kiyohiko

AU - Toader, Elena

AU - Valentová, Kateřina

AU - Vertzoni, Maria

AU - De Wildt, Saskia

AU - Wilson, Clive G

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N2 - 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.

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KW - Specific patient populations

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DO - 10.1016/j.addr.2021.02.001

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

Access to Document

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Cite this