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.authorIlie, Alexandra-Roxana
dc.contributor.authorGriffin, Brendan T.
dc.contributor.authorBrandl, Martin
dc.contributor.authorBauer-Brandl, Annette
dc.contributor.authorJacobsen, Ann-Christin
dc.contributor.authorVertzoni, Maria
dc.contributor.authorKuentz, Martin
dc.contributor.authorKolakovic, Ruzica
dc.contributor.authorHolm, René
dc.contributor.funderHorizon 2020en
dc.contributor.funderEuropean Cooperation in Science and Technologyen
dc.date.accessioned2020-07-14T09:37:05Z
dc.date.available2020-07-14T09:37:05Z
dc.date.issued2020-07-03
dc.date.updated2020-07-14T09:15:55Z
dc.description.abstractSupersaturated 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.sponsorshipEuropean Cooperation in Science and Technology (CA16205 - European Network on Understanding Gastrointestinal Absorption-related Processes)en
dc.description.statusPeer revieweden
dc.description.versionPublished Versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.articleid105452en
dc.identifier.citationIlie, 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.2020.105452en
dc.identifier.doi10.1016/j.ejps.2020.105452en
dc.identifier.eissn1879-0720
dc.identifier.endpage11en
dc.identifier.issn0928-0987
dc.identifier.journaltitleEuropean Journal of Pharmaceutical Sciencesen
dc.identifier.startpage1en
dc.identifier.urihttps://hdl.handle.net/10468/10247
dc.identifier.volume152en
dc.language.isoenen
dc.publisherElsevier B.V.en
dc.relation.projectinfo: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/PEARRLen
dc.relation.urihttp://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.urihttps://creativecommons.org/licenses/by/4.0/en
dc.subjectSupersaturated lipid-based drug delivery systemsen
dc.subjectDrug permeabilityen
dc.subjectSteady-state fluxen
dc.subjectDynamic permeation modelen
dc.subjectIn vivo pharmacokineticsen
dc.titleExploring impact of supersaturated lipid-based drug delivery systems of celecoxib on in vitro permeation across PermeapadⓇ membrane and in vivo absorptionen
dc.typeArticle (peer-reviewed)en
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