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.check.date2021-01-24
dc.check.infoAccess to this article is restricted until 12 months after publication by request of the publisher.en
dc.contributor.authorIlie, Alexandra-Roxana
dc.contributor.authorGriffin, Brendan T.
dc.contributor.authorKolakovic, Ruzica
dc.contributor.authorVertzoni, Maria
dc.contributor.authorKuentz, Martin
dc.contributor.authorHolm, René
dc.contributor.funderHorizon 2020en
dc.date.accessioned2020-02-05T14:59:13Z
dc.date.available2020-02-05T14:59:13Z
dc.date.issued2020-01-24
dc.date.updated2020-02-05T14:35:21Z
dc.description.abstractObjective: 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.description.statusPeer revieweden
dc.description.versionAccepted Versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.citationIlie, 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: 10.1080/03639045.2020.1721526en
dc.identifier.doi10.1080/03639045.2020.1721526en
dc.identifier.endpage29en
dc.identifier.issn0363-9045
dc.identifier.journaltitleDrug Development and Industrial Pharmacyen
dc.identifier.startpage1en
dc.identifier.urihttps://hdl.handle.net/10468/9614
dc.language.isoenen
dc.publisherTaylor & Francisen
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.urihttps://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/10.1080/03639045.2020.1721526en
dc.subjectSupersaturated lipid-based drug delivery systemsen
dc.subjectPre-formulationen
dc.subjectSolubility screeningen
dc.subjectFormulation developmenten
dc.subjectPhysical stabilityen
dc.titleSupersaturated lipid-based drug delivery systems – exploring impact of lipid composition type and drug properties on supersaturability and physical stabilityen
dc.typeArticle (peer-reviewed)en
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