Heat induced evaporative antisolvent nanoprecipitation (HIEAN) of itraconazole.
Item Type:Journal Article
Citation:Mugheirbi NA, Paluch KJ, Tajber L, Heat induced evaporative antisolvent nanoprecipitation (HIEAN) of itraconazole., International Journal of Pharmaceutics, 471, 1-2, 2014, 400 - 411
HIEAN_ITR.pdf (Accepted for publication (author's copy) - Peer Reviewed) 3.885Mb
traconazole (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 gastro-intestinal conditions when compared to amorphous ITR microparticles. The incorporation of 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.
Author: TAJBER, LIDIA
Type of material:Journal Article
Series/Report no:International Journal of Pharmaceutics
Availability:Full text available
Subject (TCD):Immunology, Inflammation & Infection , Nanoscience & Materials , Nanopharmacy , Pharmacy