Supersaturated lipid-based drug delivery systems – exploring impact of lipid composition type and drug properties on supersaturability and physical stability

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dc.contributor.author Ilie, Alexandra-Roxana
dc.contributor.author Griffin, Brendan T.
dc.contributor.author Kolakovic, Ruzica
dc.contributor.author Vertzoni, Maria
dc.contributor.author Kuentz, Martin
dc.contributor.author Holm, René
dc.date.accessioned 2020-02-05T14:59:13Z
dc.date.available 2020-02-05T14:59:13Z
dc.date.issued 2020-01-24
dc.identifier.citation Ilie, A.-R., Griffin, B. T., Kolakovic, R., Vertzoni, M., Kuentz, M. and Holm, R. (2020) 'Supersaturated lipid-based drug delivery systems – exploring impact of lipid composition type and drug properties on supersaturability and physical stability', Drug Development and Industrial Pharmacy, pp. 1-29. doi: 10.1080/03639045.2020.1721526 en
dc.identifier.startpage 1 en
dc.identifier.endpage 29 en
dc.identifier.issn 0363-9045
dc.identifier.uri http://hdl.handle.net/10468/9614
dc.identifier.doi 10.1080/03639045.2020.1721526 en
dc.description.abstract Objective: The objective of the current study was to systematically investigate the impact of lipid composition on the ability to design supersaturated lipid-based drug delivery systems (sLBDDS) using three model drugs with different physico-chemical properties. Significance: This study expands the list of investigated sLBDDS by using alternative vehicle compositions relative to current literature. Methods & Results: Drug supersaturation was thermally-induced based on previously reported methods and was successfully achieved for celecoxib and cinnarizine. For the novel drug, JNJ-2A, a lower supersaturation potential was observed for the tested LBDDS. For celecoxib and cinnarizine, crystalline precipitate was observed for some sLBDDS upon storage at 25 °C/65%RH, particularly for medium chain sLBDDS (celecoxib) and long chain sLBDDS (cinnarizine). The greater risk of precipitation observed for celecoxib and cinnarizine, particularly at higher apparent degree of supersaturation (aDS) may be related to their higher crystallization tendency as determined by differential scanning calorimetry. Conclusions: In conclusion, the potential for supersaturation in LBDDS, and the risk of precipitation, was found to be highly drug dependent. The apparent degree of supersaturation was considered a major factor impacting the ability to maintain drug supersaturation upon storage. 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/10.1080/03639045.2020.1721526
dc.rights © 2020 Informa UK Limited. This is an Accepted Manuscript of an article published by Taylor & Francis in Drug Development and Industrial Pharmacy on 24 January 2020, available online: http://www.tandfonline.com/10.1080/03639045.2020.1721526 en
dc.subject Supersaturated lipid-based drug delivery systems en
dc.subject Pre-formulation en
dc.subject Solubility screening en
dc.subject Formulation development en
dc.subject Physical stability en
dc.title Supersaturated lipid-based drug delivery systems – exploring impact of lipid composition type and drug properties on supersaturability and physical stability 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 2021-01-24
dc.date.updated 2020-02-05T14:35:21Z
dc.description.version Accepted Version en
dc.internal.rssid 501545254
dc.contributor.funder Horizon 2020 en
dc.description.status Peer reviewed en
dc.identifier.journaltitle Drug Development and Industrial Pharmacy en
dc.internal.copyrightchecked No
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress brendan.griffin@ucc.ie en
dc.internal.bibliocheck In press. Check vol / issue / page range. Update citation, rights statement 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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