Abstract:
This research was designed to optimize itraconazole-loaded polyisobutyl- cyanoacrylate (PIBCA) nanoparticles and itraconazole-loaded poly (lactide-co-glycolide) (PLGA) using factorial designs and response surface methodology. In this study the stability and cytotoxicity of both nanoparticles were also investigated. A validated statistical model having significant coefficient figures (P < 0.05) for the particle size, particle size distribution, amount of itraconazole entrapped in the nanoparticles, and encapsulation efficiency as function of the polymer or monomer, benzyl benzoate, and itraconazole were developed. Multiple response optimizations by using the overlay contour plot for the responses and the desirability approach allowed the selection of the optimum formulation ingredients for nanoparticles containing itraconazole of 500 microgram/mL. The composition of itraconazole-loaded PLGA nanoparticles contained 10 mg/mL of PLGA, 16.94 microgram/mL of benzyl benzoate and 1001.01 microgram/mL of itraconazole whereas the composition of itraconazole-loaded PIBCA nanoparticles contained 8.09 microlitre/mL of IBCA, 10.19 microgram/mL of benzyl benzoate and 1200.77 microgram/mL of itraconazole. Factorial designs and response surface methodology have been successfully used to construct a statistical model for the particle size, polydispersity index and encapsulation efficiency as a function of the formulation variables. The optimized formula of itraconazole-loaded PIBCA nanoparticles was more stable than the optimized formula of itraconazole-loaded PLGA nanoparticles. On the contrary, the cytotoxicity of plain and itraconazole-loaded PLGA nanoparticles was less prominent than that of plain and itraconazole-loaded PIBCA nanoparticles. The estimated IC[subscript 50] values of PLGA nanoparticles and PIBCA nanoparticles were 79.2 mg/mL and 114 microgram/mL, respectively
