Abstract:
The objective of the study was to design and evaluate Itraconazole loaded solid lipid nanoparticles (SLNs) drug
delivery system, where Itraconazole nanoparticles with suitable size ranges are expected to improve the
therapeutic efficacy and reduction of toxicity of this broad spectrum antifungal agent. Components of the SLNs
were lipid (palmitic acid) and surfactants (Pluronic F127 and Tween 40). The Itraconazole loaded nanoparticles
were prepared by microemulsion dispersion method. Experiments were carried out with optimized ratio of
excipients, where drug-lipid ratio and surfactant-cosurfactant ratio (Km) were varied to optimize the
formulation characteristics. The effects of dispersion media, its pH, ionic content, etc. were investigated to
optimize the SLNs production. Particles size analysis and zeta potential measurements were done using
Malvern Mastersizer Hydro 2000G. The particles were also subjected to DSC, IR and XRD analyses. The in
vitro drug release profile from nanoparticles was found to prolong up to 12h. Kinetic analysis of release
indicated that nanoparticles formed were matrix in nature, in which Itraconazole dispersed uniformly.
Optimized formulations were found to have a lipid-drug ratio of 1.5:1 and prepared at a Km ratio of 1:2 to
maximize drug loading, modulate release and minimized particle size. The microemulsion mediated
nanoparticle preparation methodology ensured high drug loading (ca. 80%), low and narrow size distribution
and provided a reproducible and fast production method. The study elaborates on the feasibility and suitability
of lipid based colloidal drug delivery system, employing optimize design to develop a clinically useful
nanoparticle system with targeting potential.
