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Impact of solidification on the performance of lipid-based colloidal carriers: oil-based versus self-emulsifying systems

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dc.contributor.authorAlinaghi, A.
dc.contributor.authorTan, A.
dc.contributor.authorRao, S.
dc.contributor.authorPrestidge, C.A.
dc.date.issued2015
dc.descriptionLink to a related website: http://pdfs.semanticscholar.org/3492/1b15daa9df49a60fb22c5fddfc4896a0e49d.pdf, Open Access via Unpaywall
dc.description.abstractThe study aims to develop and optimise lipid-based colloidal carriers (LBCC) for enhancing solubilisation and reducing fed/fasted variation for the poorly water-soluble danazol (DAN). Oil-based and self-microemulsifying delivery systems (SMEDDS) were developed, and the effect of solidification was investigated. Liquid SMEDDS (L-SMEDDS, Capmul MCM:Tween 80:Transcutol HP 1:2:1, w/w) and emulsion (Capmul MCM:soya lecithin 100:0.6, w/w) were developed. Solid-state formulations were prepared via (i) physical adsorption of L-SMEDDS (P-SMEDDS) or (ii) spray drying of emulsion (silica-lipid hybrid, SLH) and L-SMEDDS (spray-dried SMEDDS, S-SMEDDS) using Aerosil 380 silica nanoparticles as the solid carrier. In vitro lipid digestion and drug solubilisation under simulated intestinal conditions in both fasted and fed states were investigated. Solubilisation of unformulated DAN under both fasted and fed conditions was low, and a large fed/fasted variation was observed, i.e. 6.6-fold difference. All LBCC formulations provided enhanced drug solubilisation and significantly reduced the fed/fasted variation. For self-emulsifying LBCC, the fasted state drug solubilisation was ranked as L-SMEDDS > PSMEDDS > S-SMEDDS, suggesting that solidification reduced the capability of SMEDDS in presenting DAN to the aqueous phase. However, in the case of oil-based LBCC, improved drug solubility was observed with the solid form SLH under both fasted and fed state in comparison to that of the equivalent liquid form. Overall, the SLH, which provided the highest drug solubilisation in the fasted state (i.e. 10-fold higher than the pure DAN) and the smallest fed/fasted variation, was considered an optimised solid LBCC to enhance the solubilisation of DAN and reduce the fed/fasted variation.
dc.identifier.citationCurrent Drug Delivery, 2015; 12(1):16-25
dc.identifier.doi10.2174/1567201811666140716122644
dc.identifier.issn1567-2018
dc.identifier.issn1875-5704
dc.identifier.urihttps://hdl.handle.net/11541.2/115206
dc.language.isoen
dc.publisherBentham Science Publishers
dc.relation.fundingARC
dc.relation.fundingNHMRC
dc.relation.fundingITEK Pty. Ltd.
dc.relation.fundingBio-innovation South Australia
dc.relation.fundingAustralian Biotech Ceridia Pty. Ltd.
dc.rightsCopyright 2015 Bentham Science Publishers
dc.source.urihttps://doi.org/10.2174/1567201811666140716122644
dc.subjectcolloidal carriers
dc.subjectfasted state
dc.subjectfed state
dc.subjectfood effect
dc.subjectin vitro lipolysis
dc.subjectlipid-based
dc.subjectself-microemulsifying
dc.subjectsilicalipid hybrid
dc.titleImpact of solidification on the performance of lipid-based colloidal carriers: oil-based versus self-emulsifying systems
dc.typeJournal article
pubs.publication-statusPublished
ror.mmsid9915930100201831

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