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dc.contributor.authorShamsi, S.
dc.contributor.authorChen, Yan
dc.contributor.authorLim, L.
dc.date.accessioned2017-01-30T15:00:46Z
dc.date.available2017-01-30T15:00:46Z
dc.date.created2015-12-10T04:25:56Z
dc.date.issued2015
dc.date.submitted2015-12-10
dc.identifier.citationShamsi, S. and Chen, Y. and Lim, L. 2015. Characterization and biological properties of NanoCUR formulation and its effect on major human cytochrome P450 enzymes. International Journal of Pharmaceutics. 495 (1): pp. 194-203.
dc.identifier.urihttp://hdl.handle.net/20.500.11937/42605
dc.identifier.doi10.1016/j.ijpharm.2015.08.066
dc.description.abstract

© 2015 Elsevier B.V. All rights reserved. Curcumin (CUR) has been formulated into a host of nano-sized formulations in a bid to improve its in vivo solubility, stability and bioavailability. The aim of this study was to investigate whether the encapsulation of CUR in nanocarriers would impede its biological interactivity, specifically its potential anti-cancer adjuvant activity via the modulation of CYP enzymes in vitro. NanoCUR, a micellar dispersion prepared via a thin film method using only Pluronic F127 as excipient, was amenable to lyophilization, and retained its nano-sized spherical dimensions (17-33 nm) upon reconstitution with water followed by dilution to 5 µM with HBSS or EMEM. NanoCUR was a weaker cytotoxic agent compared to CUR in solution (sCUR), affecting HepG2 cell viability only when the incubation time was prolonged from 4 h to 48 h. Correlation with 2 h uptake data suggests this was due to a lower cellular uptake rate of CUR from NanoCUR than from sCUR. The poorer CUR accessibility might also account for NanoCUR being a weaker inhibitor of CYP2C9 and CYP2D6 than sCUR. NanoCUR was, however, 1.76-fold more potent against the CYP3A4 (IC<inf>50</inf> 5.13 ± 0.91 µM) metabolic function. The higher activity against CYP3A4 might be attributed to the synergistic action of Pluronic F127, since the blank micellar dispersion also inhibited CYP3A4 activity. Both sCUR and NanoCUR had no effect on the CYP3A4 mRNA levels in the HepG2 cells. NanoCUR therefore, maintained most of the biological activities of CUR in vitro, albeit at a lower potency and response rate.

dc.publisherElsevier
dc.titleCharacterization and biological properties of NanoCUR formulation and its effect on major human cytochrome P450 enzymes
dc.typeJournal Article
dcterms.dateSubmitted2015-12-10
dcterms.source.volume495
dcterms.source.number1
dcterms.source.startPage194
dcterms.source.endPage203
dcterms.source.issn0378-5173
dcterms.source.titleInternational Journal of Pharmaceutics
curtin.digitool.pid234559
curtin.pubStatusPublished
curtin.refereedTRUE
curtin.departmentSchool of Pharmacy
curtin.identifier.scriptidPUB-HEA-SPM-YC-26276
curtin.identifier.elementsidELEMENTS-95840
curtin.accessStatusFulltext not available


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