Formulation Characterization and Optimization of Chitosan Nanoparticles Loaded with Sorafenib Tosylate

Author(s)

Dileep, K.J., Rajesh, R., Nair, C.R.S.

Author's Affiliation

Abstract

Chitosan is a biocompatible natural polymer used extensively for fabrication of nanoparticles with the aim of safe and efficient drug delivery. Sorafenib, is an orally active bi-aryl urea compound that inhibits cell proliferation by multikinase inhibition and reported to be effective in the treatment of hepatocellular carcinoma. The clinical application of this drug is limited by its decreased bioavailability. Use of biocompatible nanoparticles as drug delivery system is a possible alternative to avoid this limitation and with this objective the present investigation concerns with the development, characterization and optimization of chitosan nanoparticles loaded with sorafenib tosylate based on 2³ full factorial design experimentation. Three independent process factors namely concentration of chitosan, amount of drug added and the pH were selected for the study. Relationship and effect of these factors on two responses, encapsulation efficiency and percentage yield, were used to characterize and optimize the nanoparticle formulation.  The significance of combinations were analysed by ANOVA and p values. Production of discrete nanoparticles below 20nm size was confirmed by performing TEM analysis. Contour plots and three dimensional surface response plots were drawn to evaluate the interaction of independent variable on the chosen dependent variables. Maximum encapsulation efficiency of 30.16% was obtained for nanoparticles prepared with a combination of 1.25 mg/ml chitosan concentration, pH 4.5 and 10 mg of sorafenib tosylate.

Keywords

Chitosan, nanoparticles, sorafenib tosylate, factorial design, TEM, HPLC, DSC

Cite This Article

Dileep, K.J., Rajesh, R., & Nair, C.R.S. (2016). Formulation Characterization and Optimization of Chitosan Nanoparticles Loaded with Sorafenib Tosylate, International Journal for Pharmaceutical Research Scholars (IJPRS), 5(1), 180-191.