Trends in the Assessment of Drug Supersaturation and Precipitation In Vitro Using Lipid-Based Delivery Systems

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Authors
Stillhart, Cordula
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Publication date
2016
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01A - Journal article
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Parent work
Journal of Pharmaceutical Sciences
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DOI of the original publication
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Series number
Volume
105
Issue / Number
9
Pages / Duration
2468-2476
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Elsevier
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Abstract
The generation of drug supersaturation close to the absorptive site is an important mechanism of how several formulation technologies enhance oral absorption and bioavailability. Lipid-based formulations belong to the supersaturating drug delivery systems although this is not the only mechanism of how drug absorption is promoted in vivo. Different methods to determine drug supersaturation and precipitation from lipid-based formulations are described in the literature. Experimental in vitro setups vary according to their complexity and proximity to the in vivo conditions and, therefore, some tests are used for early formulation screening, while others better qualify for a later stage of development. The present commentary discusses this rapidly evolving field of in vitro testing with a special focus on the advancements in analytical techniques and new approaches of mechanistic modeling. The importance of considering a drug absorption sink is particularly emphasized. This commentary should help formulators in the pharmaceutical industry as well as in academia to make informed decisions on how to conduct in vitro tests for lipid-based delivery systems and to decide on the implications of experimental results.
Keywords
absorption, supersaturation, bioavailability, lipids, mathematical model
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ISBN
ISSN
0022-3549
1520-6017
Language
English
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Yes
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Publication status
Published
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Peer review of the complete publication
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License
Citation
STILLHART, Cordula und Martin KUENTZ, 2016. Trends in the Assessment of Drug Supersaturation and Precipitation In Vitro Using Lipid-Based Delivery Systems. Journal of Pharmaceutical Sciences. 2016. Bd. 105, Nr. 9, S. 2468–2476. DOI 10.1016/j.xphs.2016.01.010. Verfügbar unter: http://hdl.handle.net/11654/23725