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dc.contributor.authorMugheirbi, N.A.*
dc.contributor.authorPaluch, Krzysztof J.*
dc.contributor.authorTajber, L.*
dc.date.accessioned2017-11-08T11:37:33Z
dc.date.available2017-11-08T11:37:33Z
dc.date.issued2014-08
dc.identifier.citationMugheirbi NA, Paluch KJ and Tajber L (2014) Heat induced evaporate antisolvent nanoprecipitation (HIEAN) of itraconazole. International Journal of Pharmaceutics. 471(1-2): 400- 411.en_US
dc.identifier.urihttp://hdl.handle.net/10454/13702
dc.descriptionYesen_US
dc.description.abstractItraconazole (ITR) is an antifungal drug with a limited bioavailability due to its poor aqueous solubility. In this study, ITR was used to investigate the impact of nanonisation and solid state change on drug’s apparent solubility and dissolution. A bottom up approach to the production of amorphous ITR nanoparticles (NPs), composed of 100% drug, with a particle diameter below 250 nm, using heat induced evaporative antisolvent nanoprecipitation (HIEAN) from acetone was developed. The NPs demonstrated improved solubility and dissolution in simulated gastrointestinal conditions when compared to amorphous ITR microparticles. NPs produced with polyethylene glycol (PEG) or its methoxylated derivative (MPEG) as a stabiliser enabled the production of smaller NPs with narrower particle size distribution and enhanced apparent solubility. MPEG stabilised NPs gave the greatest ITR supersaturation levels (up to 11.6 ± 0.5 μg/ml) in simulated gastric fluids. The stabilising polymer was in an amorphous state. Dynamic vapour sorption data indicated no solid state changes in NP samples with water vapour at 25 °C, while crystallisation was apparent at 50 °C. HIEAN proved to be an efficient method of production of amorphous ITR NPs, with or without addition of a polymeric stabiliser, with enhanced pharmaceutical properties.en_US
dc.description.sponsorshipLibyan Ministry of Higher Education and Scientific Research through the Libyan Embassy, London and supported by the Science Foundation Ireland under Grant No. 12/RC/2275 (Synthesis and Solid State Pharmaceuticals Centre).en_US
dc.language.isoenen_US
dc.relation.isreferencedbyhttps://doi.org/10.1016/j.ijpharm.2014.05.045en_US
dc.rights© 2014 Elsevier. Reproduced in accordance with the publisher's selfarchiving policy. This manuscript version is made available under the CC-BY-NC-ND 4.0 license.en_US
dc.subjectItraconazole; Poly(ethylene glycol); Methoxylated poly(ethylene glycol); Antisolvent evaporative nanoprecipitation; Nanoparticles; Amorphousen_US
dc.titleHeat induced evaporative antisolvent nanoprecipitation (HIEAN) of itraconazoleen_US
dc.status.refereedYesen_US
dc.date.Accepted2014-05-26
dc.date.application2014-05-29
dc.typeArticleen_US
dc.type.versionAccepted Manuscripten_US
refterms.dateFOA2018-07-29T02:41:06Z


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