In vitro digestion models to evaluate lipid based drug delivery systems; present status and current trends
Abstract
During the past two decades, a range of in vitro models simulating the digestion processes occurring in the stomach and small intestine have been developed to characterize lipid based drug delivery systems (LbDDSs). This review describes the presently existing range of in vitro digestion models and their use in the field of oral drug delivery. The models are evaluated in terms of their suitability to assess LbDDSs, and their ability to produce in vitro - in vivo correlations (IVIVCs). While the pH-stat lipolysis model is by far the most commonly utilized in vitro digestion model in relation to characterizing LbDDSs, a series of recent studies have shown a lack of IVIVCs limiting its future use. Presently, no single in vitro digestion model exists which is able to predict the in vivo performance of various LbDDSs. However, recent research has shown the potential of combined digestion-permeation models as well as species specific digestion models.
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Digestion plays an important role in absorption processes of poorly water-soluble drugs from lipid-based drug delivery systems.
“Digestion is believed to play an important role in absorption processes of PWSD from LBDDS, which has guided research towards establishing increasingly complex lipolysis models (Iwanaga et al., 2006; Yeap et al., 2013; Berthelsen et al., 2019).”
From Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption (2020) · cites this paper as Berthelsen et al., 2019
Cites
From Sewer to Saviour—Targeting the Lymphatic System to Promote Drug Exposure and Activity
Trevaskis, N. L., Kaminskas, L. M., & Porter, C. J. H. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4608 · Cited by 654 · see citing works
50 years of oral lipid-based formulations: provenance, progress and future perspectives
Feeney, O. M., Crum, M. F., McEvoy, C. L., Trevaskis, N. L., Williams, H. D., Pouton, C. W., Charman, W. N., Bergström, C. A. S., & Porter, C. J. H. (2016) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2016.04.007 · Cited by 426 · see citing works
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Ilie, A.-R., Griffin, B. T., Brandl, M., Bauer-Brandl, A., Jacobsen, A.-C., Vertzoni, M., Kuentz, M., Kolakovic, R., & Holm, R. (2020) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2020.105452 · Cited by 33 · see citing works
- Authors
- Berthelsen, R., Klitgaard, M., Rades, T., & Müllertz, A.
- Affiliations
- University of Copenhagen (DK)
- Corresponding author
- Berthelsen, Ragna
- Venue
- Advanced Drug Delivery Reviews
- Publisher
- Elsevier BV
- Published
- 2019-03
- Volume
- 142
- Pages
- 35-49
- ISSN
- 0169-409X (ISSN-L)
- OpenAlex
- W2954412771
- Cited by
- 111
- References
- 2
- Citations by year
- 2026: 11 · 2025: 13 · 2024: 10 · 2023: 13 · 2022: 22 · 2021: 24 · 2020: 17 · 2019: 1
- FWCI
- 1.52
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Advanced Drug Delivery Reviews (publishedVersion)
- PubMed (publishedVersion)
- Research at the University of Copenhagen (University of Copenhagen) (submittedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Agricultural and Biological Sciences › Food Science › Proteins in Food Systems
- Keywords
- in vitro digestion model, lipid-based drug delivery, oral drug delivery, in vitro-in vivo correlation, gastrointestinal digestion simulation, lipolysis
- MeSH terms
- Animals, Digestion, Humans, Lipids, Models, Biological, Drug Delivery Systems, Gastrointestinal Tract
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