Formulation development and characterization of chitosan nanoparticles of montelukast sodium for site specific drug delivery in anagement of asthma

Abstract

Targeted delivery of drug molecule to lungs is being explored as an avenue for better & faster relief from pulmonary disorders. Montelukast sodium (MS), a leukotrine receptor antagonist (LTRA) used for the maintenance therapy of asthma & providing symptomatic relief from seasonal allergies, in conventional formulation undergoes major hepatic first pass metabolism, decreasing bioavailability to 64%. The objective of the present investigation was to formulate free flowing, respirable, biodegradable chitosan nanoparticles (NPs) for controlled delivery of MS to broncho alveolar tract for management of asthma. NPs loaded with MS were prepared by Ionic gelation method. The effect of chitosan concentration & mass ratio of chitosan: Tri poly Phosphate (TPP) was optimized on the basis of particle size, zeta potential, and % entrapment efficiency (%EE). From the results, it was observed that as the chitosan concentration increased from 0.25 to 0.85%, the particle size linearly increased with a decrease in zeta potential & %EE. However, as chitosan: TPP mass ratio was increased no significant effect on particle size & zeta potential was observed. Drug release from NPs was found to be influenced by long chain chitosan segments, chitosan: TPP mass ratio and initial burst effect, due to superficial presence of drug particles. Nanoparticulate formulation with optimized concentration of chitosan, and optimized chitosan: TPP mass ratio shows particle size of 222.5 nm, zeta potential +24.9 and %EE 61.8%. All these attributes render the optimized Montelukast loaded Chitosan Nanoparticles may be considered as promising for developed DPI of MS