Development and Characterisation of Itraconazole Loaded Nanostructured Lipid Carrier for Delivery Across the Blood-Brain Barrier

Abstract

The objectives of this study were to develop and characterise itraconazole loaded nanostructured lipid carrier (ITZ-NLC) and to study their potential for drug delivery into the brain. Precirol ATO 5 and Transcutol HP were selected as the lipid phase, Tween 80 and Solutol HS15 as surfactants. The ITZ-NLC was prepared by hot homogenisation and high pressure homogeniser method. The entrapment efficiency for the best formulation batch was analysed using high performance liquid chromatography method and was found to be 70.5±0.6%. The average size and zeta potential for the ITZ-NLC was 313.7±15.3nm and −18.7±0.3mV respectively. Transmission electron microscope study confirms ITZ-NLC is spherical shape. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ encapsulated in NLC was present in the amorphous form. In vitro release study showed that ITZ-NLC achieved a sustained release with cumulative release of 80.6±5.3% up to 24 hour. Results from in vivo study showed that ITZ-NLC can increase the ITZ brain concentration for almost 2-fold. These results suggested that ITZ-NLC can be exploited as a potential nanocarrier to achieve sustained release and brain targeted delivery.