Optimization of Site-Specific Drug Delivery System of Tyrosine Kinase Inhibitor Using Response Surface Methodology

Aims: The aim of present study was to develop a stomach specific formulation of Imatinibmesylate to increase the fraction of drug absorbed in stomach.

Study Design: Development and Optimization of Microspheres for site specific delivery..

Place and Duration of Study: The study was carried out in Department of Pharmacy, Annamalai University, between October 2020 and July 2021.

Methodology: Ionotropic gelation method with Sodium alginate and Chitosan were used to formulate the mucoadhesive microspheres with calcium chloride. The formulation was optimized using Box – Behnken design to study the effect of independent variables, Amount of Sodium Alginate (X1), Amount of Chitosan (X2) and concentration of Calcium Chloride (X3) on dependent variables Particle Size (Y1), Entrapment Efficiency (Y2) and In-vitro drug release (Y3).

Results: Particle size of prepared microspheres varied from 458.25 to 810.75 μm, entrapment efficiency from 64.87 to 82.63% and in-vitro release from 69.22 to 83.50%. The optimized formulation was found using point prediction, and formulation showed optimum results. The drug release was controlled for more than 12 h.

Conclusion: Stomach specific formulation of Imatinibmesylate was successfully optimized by a three-factor, three level Box – Behnken design.