Design and Characterization of Mesalamine Loaded Nanoparticles for Controlled Delivery System

Objective(s): Nanoparticles (NPs) are known for their specific accumulation in the inflamed tissues of the colon and thus allow a selective delivery to the site of inflammation with minimum adverse effects. The main objective of this work is to attain mesalamine loaded chitosan nanoparticles as a carrier for oral delivery. Methods: In this study, mesalamine loaded chitosan nanoparticles were prepared using an ionic gelation method. Experimental design Box-Behnken response surface methodology was used for the optimization of the nanoparticles. The nanoparticles size and gelation process of the polymeric nano-drug controlled release system depends on several variables including the concentration ratio of chitosan-TPP, concentration of mesalamine, concentration of chitosan solution and pH of the solution with optimum conditions of 2.3, 0.02 mg/ml, 0.1 mg/ml and 4.5, respectively. Moreover, the morphology of the prepared nanoparticles was observed by scanning electron microscopy (SEM). Also, characterization of the chitosan-mesalamine nanoparticles was performed by FT-IR spectrophotometer for specifying the chemical structure of nanoparticles molecules and differential scanning calorimetry (DSC) for studying thermal behavior. Drug release profile and the amount of the loaded drug were also monitored by UV-Vis spectroscopy. Results: The mean particle size of the synthesized nanoparticles was ranging from 53.9 to 322.8 nm using a dynamic light scattering (DLS) technique. SEM image shows segregated and non-aggregated nanoparticles with sub-spherical smooth morphology. An in-vitro release study of the prepared nanoparticles illustrated that the percentage of mesalamine released from the nanoparticles was 90.17 ± 2.45% within 48 hrs. Conclusion: Drug released showed that the release profile of mesalamine loaded nanoparticles was in a slow manner and no initial rapid release (burst effect) was illustrated.