Developing an in vitro lipolysis model for real-time analysis of drug concentrations during digestion of lipid-based formulations

Simple item page
dc.contributor.authorEjskjær, Lotteen
dc.contributor.authorO'Dwyer, Patrick J.en
dc.contributor.authorRyan, Callum D.en
dc.contributor.authorHolm, Renéen
dc.contributor.authorKuentz, Martinen
dc.contributor.authorBox, Karl J.en
dc.contributor.authorGriffin, Brendan T.en
dc.contributor.funderHORIZON EUROPE Marie Sklodowska-Curie Actionsen
dc.contributor.funderHorizon 2020en
dc.date.accessioned2024-06-10T09:55:55Z
dc.date.available2024-06-10T09:55:55Z
dc.date.issued2023-12-20en
dc.description.abstractUnderstanding the effect of digestion on oral lipid-based drug formulations is a critical step in assessing the impact of the digestive process in the intestine on intraluminal drug concentrations. The classical pH-stat in vitro lipolysis technique has traditionally been applied, however, there is a need to explore the establishment of higher throughput small-scale methods. This study explores the use of alternative lipases with the aim of selecting digestion conditions that permit in-line UV detection for the determination of real-time drug concentrations. A range of immobilised and pre-dissolved lipases were assessed for digestion of lipid-based formulations and compared to digestion with the classical source of lipase, porcine pancreatin. Palatase® 20000 L, a purified liquid lipase, displayed comparable digestion kinetics to porcine pancreatin and drug concentration determined during digestion of a fenofibrate lipid-based formulation were similar between methods. In-line UV analysis using the MicroDISS ProfilerTM demonstrated that drug concentration could be monitored during one hour of dispersion and three hours of digestion for both a medium- and long-chain lipid-based formulations with corresponding results to that obtained from the classical lipolysis method. This method offers opportunities exploring the real-time dynamic drug concentration during dispersion and digestion of lipid-based formulations in a small-scale setup avoiding artifacts as a result of extensive sample preparation.en
dc.description.statusPeer revieweden
dc.description.versionPublished Versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.articleid106681en
dc.identifier.citationEjskjær, L., O’Dwyer, P.J., Ryan, C.D., Holm, R., Kuentz, M., Box, K.J. and Griffin, B.T. (2024) ‘Developing an in vitro lipolysis model for real-time analysis of drug concentrations during digestion of lipid-based formulations’, European Journal of Pharmaceutical Sciences, 194, 106681. Available at: https://doi.org/10.1016/j.ejps.2023.106681en
dc.identifier.doihttps://doi.org/10.1016/j.ejps.2023.106681en
dc.identifier.endpage10en
dc.identifier.issn0928-0987en
dc.identifier.journaltitleEuropean Journal of Pharmaceutical Sciencesen
dc.identifier.startpage1en
dc.identifier.urihttps://hdl.handle.net/10468/15995
dc.identifier.volume194en
dc.language.isoenen
dc.publisherElsevieren
dc.relation.ispartofEuropean Journal of Pharmaceutical Sciencesen
dc.relation.projectinfo:eu-repo/grantAgreement/EC/H2020::MSCA-ITN-EID/955756/EU/A fully integrated, animal-free, end-to-end modelling approach to oral drug product development/InPharmaen
dc.rights© 2023 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.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectLipid-based formulationsen
dc.subjectIn vitro lipolysisen
dc.subjectFenofibrateen
dc.subjectLipid digestionen
dc.titleDeveloping an in vitro lipolysis model for real-time analysis of drug concentrations during digestion of lipid-based formulationsen
dc.typeArticle (peer-reviewed)en
oaire.citation.volume194en
Files
Original bundle
Now showing 1 - 2 of 2
Thumbnail Image
Name:
1-s2.0-S0928098723003093-main.pdf
Size:
1.78 MB
Format:
Adobe Portable Document Format
Description:
Published version
Download
Thumbnail Image
Name:
1-s2.0-S0928098723003093-mmc1.docx
Size:
573.32 KB
Format:
Microsoft Word XML
Description:
Supplementary materials
Download
License bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
license.txt
Size:
2.71 KB
Format:
Item-specific license agreed upon to submission
Description:
Download
Collections
Pharmacy - Journal Articles