Design and evaluation of itraconazole loaded solid lipid nanoparticulate system for improving the antifungal therapy

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

Design and optimization of nsaid loaded nanoparticles

The objective of the study was to design and evaluate NSAID loaded Nanoparticles drug delivery system, where Flurbiprofen [model drug] Nanoparticles with suitable size range are envisaged to concentrate at inflammation sites due to increase fragility of blood vessels at those sites and increased aggregation and prostaglandin synthesis. Materials used were surfactant [pluronic F 68] and polymer [poly lactic co glycolic acid; PLGA]. The flurbiprofen loaded nanoparticles were prepared by solvent diffusion nano-precipitation method. Experiment was carried out following 32 factorial designs, where drug-polymer ratio was varied to optimize the formulation. From I.R studies no drug-polymer interaction was found. Particles size analysis was done using Malvern Mastersizer. Two parameters, namely, drug-polymer ratio and solvent-nonsolvent ratio were chosen for optimization following the factorial design. Amount of drug loading and surfactant were kept constant, and only polymer load was varied. The in-vitro drug release profile from nanoparticles was found to follow Higuchi square root kinetics implying a diffusion dependent release as is expected of an insoluble, non-swellable nature of PLGA. It indicated that nanoparticles formed were matrix in nature, in which flurbiprofen dispersed uniformly. Suitable polynomial models were generated and statistically validated using ANOVA for the different responses, namely drug release [maximization] and particle size [minimization]. Those models were solved numerically and simultaneously to optimize the required formulation. Optimized formulation were found to have a polymer-drug ratio of 18.89:1 and manufactured at a nonsolvent-solvent ratio of 4:1 to maximized release after 8 hrs and minimized particle size. The methodology avoids the use of organic solvent and thus provides a safe, reproducible and fast method of production of nanoparticles. The study collaborates on the feasibility and suitability of aqueous polymeric drug delivery system, employing statistical design to develop a clinically useful Nanoparticle system with targeting potential