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.
