High payload itraconazole‐incorporated lipid nanoparticles with modulated release property for oral and parenteral administration

Objectives The aim of this study was to develop high payload itraconazole‐incorporated lipid nanoparticles (HINP) with modulated release property using a binary mixture core of solid and liquid lipid for oral and parenteral administration. Methods High payload itraconazole‐incorporated lipid nanoparticles were prepared by hot high‐pressure homogenization method using tristearin (TS) as a solid lipid, triolein (TO) as a liquid lipid and egg phosphatidylcholine/Tween 80/DSPE‐PEG2000 as a surfactants mixture. To investigate the effects of liquid lipid in lipid core on itraconazole (ITZ) dissolution and release, TS/TO ratio was varied as 100/0, 90/10 and 80/20 (mg/mg). Key findings All HINP formulations showed particle size around 300 nm and polydispersity index below 0.3. The incorporation efficiencies of HINP formulations were above 80%, and more than 40 mg of ITZ was incorporated into each HINP formulation. In‐vitro dissolution and release rate of ITZ from HINP increased as the amount of TO in lipid core increased. Compared with commercial formulations of ITZ, the pharmacokinetics of ITZ was improved after oral and parenteral administration of HINP formulations containing 0% or 10% of TO in lipid core. Conclusion High payload itraconazole‐incorporated lipid nanoparticles with a binary mixture lipid core have a great potential for the development of controlled release formulation of ITZ.