Toward simplified oral lipid-based drug delivery using mono-/di-glycerides as single component excipients

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dc.contributor.author Ilie, Alexandra-Roxana
dc.contributor.author Griffin, Brendan T.
dc.contributor.author Vertzoni, Maria
dc.contributor.author Kuentz, Martin
dc.contributor.author Cuyckens, Filip
dc.contributor.author Wuyts, Koen
dc.contributor.author Kolakovic, Ruzica
dc.contributor.author Holm, René
dc.date.accessioned 2020-12-03T13:31:02Z
dc.date.available 2020-12-03T13:31:02Z
dc.date.issued 2020-11-09
dc.identifier.citation Ilie, A.-R., Griffin, B. T., Vertzoni, M., Kuentz, M., Cuyckens, F., Wuyts, K., Kolakovic, R. and Holm, R. (2020) 'Toward simplified oral lipid-based drug delivery using mono-/di-glycerides as single component excipients', Drug Development and Industrial Pharmacy, (10 pp). doi: 10.1080/03639045.2020.1843475 en
dc.identifier.startpage 1 en
dc.identifier.endpage 10 en
dc.identifier.issn 0363-9045
dc.identifier.uri http://hdl.handle.net/10468/10811
dc.identifier.doi 10.1080/03639045.2020.1843475 en
dc.description.abstract Objective: This study aimed to systematically explore compositional effects for a series of lipid systems, on the in vitro drug solubilization and in vivo bioavailability of three poorly water-soluble drugs with different physico-chemical properties. Significance: While many lipid-based drug products have successfully reached the market, there is still a level of uncertainty on the design guidelines for such drug products with limited understanding on the influence of composition on in vitro and in vivo performance. Methods and Results: Lipid-based drug delivery systems were prepared using either single excipient systems based on partially digested triglycerides (i.e. mono- and/or di-glycerides) or increasingly complex systems by incorporating surfactants and/or triglycerides. These lipid systems were evaluated for both in vitro and in vivo behavior. Results indicated that simple single component long chain lipid systems are more beneficial for the absorption of the weak acid celecoxib and the weak base cinnarizine compared to equivalent single component medium chain lipid systems. Similarly, a two-component system produced by incorporating small amount of hydrophilic surfactant yields similar overall pharmacokinetic effects. The lipid drug delivery systems based on medium chain lipid excipients improved the in vivo exposure of the neutral drug JNJ-2A. The higher in vivo bioavailability of long chain lipid systems compared to medium chain lipid systems was in agreement with in vitro dilution and dispersion studies for celecoxib and cinnarizine. Conclusions: The present study demonstrated the benefits of using mono-/di-glycerides as single component excipients in LBDDS to streamline formulation screening and improve oral bioavailability for the three tested poorly water-soluble drugs. en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher Taylor & Francis en
dc.relation.uri https://www.tandfonline.com/doi/full/10.1080/03639045.2020.1843475
dc.rights © 2020 Informa UK Limited, trading as Taylor & Francis Group. This is an Accepted Manuscript of an article published by Taylor & Francis in Drug Development and Industrial Pharmacy on 09 Nov 2020, available online: http://www.tandfonline.com/10.1080/03639045.2020.1843475 en
dc.subject Lipid-based drug delivery systems en
dc.subject Long versus medium chain lipid excipients en
dc.subject Biorelevant media en
dc.subject Dilution and dispersion testing en
dc.subject In vivo pharmacokinetics en
dc.title Toward simplified oral lipid-based drug delivery using mono-/di-glycerides as single component excipients en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Alexandra-Roxana Ilie, School of Pharmacy, University College Cork, Cork, Ireland. +353-21-490-3000 en
dc.internal.availability Full text available en
dc.check.info Access to this article is restricted until 12 months after publication by request of the publisher. en
dc.check.date 2021-11-09
dc.date.updated 2020-12-03T13:13:46Z
dc.description.version Accepted Version en
dc.internal.rssid 546203344
dc.contributor.funder Horizon 2020 en
dc.description.status Peer reviewed en
dc.identifier.journaltitle Drug Development and Industrial Pharmacy en
dc.internal.copyrightchecked Yes
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress brendan.griffin@ucc.ie en
dc.internal.IRISemailaddress 117223111@umail.ucc.ie 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


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