Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption

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dc.contributor.author Ilie, Alexandra-Roxana
dc.contributor.author Griffin, Brendan T.
dc.contributor.author Brandl, Martin
dc.contributor.author Bauer-Brandl, Annette
dc.contributor.author Jacobsen, Ann-Christin
dc.contributor.author Vertzoni, Maria
dc.contributor.author Kuentz, Martin
dc.contributor.author Kolakovic, Ruzica
dc.contributor.author Holm, René
dc.date.accessioned 2020-07-14T09:37:05Z
dc.date.available 2020-07-14T09:37:05Z
dc.date.issued 2020-07-03
dc.identifier.citation Ilie, A-R., Griffin, B. T., Brandl, M., Bauer-Brandl, A., Jacobsen, A.-C.; Vertzoni, M., Kuentz, M., Kolakovic, R. and Holm, R. (2020) 'Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption', European Journal of Pharmaceutical Sciences, 152, 105452 (11pp). doi: 10.1016/j.ejps.2020.105452 en
dc.identifier.volume 152 en
dc.identifier.startpage 1 en
dc.identifier.endpage 11 en
dc.identifier.issn 0928-0987
dc.identifier.uri http://hdl.handle.net/10468/10247
dc.identifier.doi 10.1016/j.ejps.2020.105452 en
dc.description.abstract Supersaturated lipid-based drug delivery systems have recently been investigated for oral administration for a variety of lipophilic drugs and have shown either equivalent or superior oral bioavailability compared to conventional non-supersaturated lipid-based drug delivery systems. The aim of the present work was to explore supersaturated versus non-supersaturated lipid-based systems at equivalent lipid doses, on in vivo bioavailability in rats and on in vitro permeation across a biomimetic PermeapadⓇ membrane to establish a potential in vivo - in vitro correlation. A secondary objective was to investigate the influence of lipid composition on in vitro and in vivo performance of lipid systems. Results obtained indicated that increasing the celecoxib load in the lipid-based formulations by thermally-induced supersaturation resulted in increased bioavailability for medium and long chain mono-/di-glycerides systems relative to their non-supersaturated (i.e. 85%) reference formulations, albeit only significant for the medium chain systems. Long chain systems displayed higher celecoxib bioavailability than equivalent medium chain systems, both at supersaturated and non-supersaturated drug loads. In vitro passive permeation of celecoxib was studied using both steady-state and dynamic conditions and correlated well with in vivo pharmacokinetic results with respect to compositional effects. In contrast, permeation studies indicated that flux and percentage permeated of supersaturated systems, either at steady-state or under dynamic conditions, decreased or were unchanged relative to non-supersaturated systems. This study has shown that by using two cell-free PermeapadⓇ permeation models coupled with rat-adapted gastro-intestinal conditions, bio-predictive in vitro tools can be developed to be reflective of in vivo scenarios. With further optimization, such models could be successfully used in pharmaceutical industry settings to rapidly screen various prototype formulations prior to animal studies. en
dc.description.sponsorship European Cooperation in Science and Technology (CA16205 - European Network on Understanding Gastrointestinal Absorption-related Processes) en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher Elsevier B.V. en
dc.relation.uri http://www.sciencedirect.com/science/article/pii/S0928098720302414
dc.rights © 2020, the Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/BY/4.0/) en
dc.rights.uri https://creativecommons.org/licenses/by/4.0/ en
dc.subject Supersaturated lipid-based drug delivery systems en
dc.subject Drug permeability en
dc.subject Steady-state flux en
dc.subject Dynamic permeation model en
dc.subject In vivo pharmacokinetics en
dc.title Exploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorption en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Brendan Griffin, Pharmacy, University College Cork, Cork, Ireland. +353-21-490-3000 Email: brendan.griffin@ucc.ie en
dc.internal.availability Full text available en
dc.date.updated 2020-07-14T09:15:55Z
dc.description.version Published Version en
dc.internal.rssid 525042418
dc.contributor.funder Horizon 2020 en
dc.contributor.funder European Cooperation in Science and Technology en
dc.description.status Peer reviewed en
dc.identifier.journaltitle European Journal of Pharmaceutical Sciences en
dc.internal.copyrightchecked Yes
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress brendan.griffin@ucc.ie en
dc.identifier.articleid 105452 en
dc.relation.project info:eu-repo/grantAgreement/EC/H2020::MSCA-ITN-ETN/674909/EU/Pharmaceutical Education And Research with Regulatory Links: Innovative drug development strategies and regulatory tools tailored to facilitate earlier access to medicines/PEARRL en
dc.identifier.eissn 1879-0720


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© 2020, the Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/BY/4.0/) Except where otherwise noted, this item's license is described as © 2020, the Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/BY/4.0/)
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