Atenolol Microparticles by Two-Factor Two-Level Central Composite Design

Abstract

Objective: The objective of this research was to formulation, optimization, and evaluation of gastric-mucoadhesive microparticles which contains selective β1 receptor antagonist atenolol.
 Methods: The following chemicals were used, atenolol (Gangwal Chemicals Pvt. Ltd., Mumbai), ethyl cellulose (EC) (Loba Chemie Pvt. Ltd., Mumbai), Carbopol 940 (Loba Chemie Pvt. Ltd., Mumbai), liquid paraffin (Arora Pharmaceuticals Pvt. Ltd., New Delhi), and Span 80 (Central Drug House (P) Ltd., New Delhi). Microparticles were prepared by the emulsification solvent evaporation technique using polymers of Carbomer 934p (CP) and EC. Disc formulations were prepared by direct compression technique from microparticles. Microparticles of combined polymers were designed according to 22 factorial central composite design (CCD), taking EC concentration and surfactant concentration as the independent variables. A total of 13 batches were prepared. The dependent variables were percentage of % drug released and % entrapment efficiency.
 Results and Discussion: All evaluation tests were done for the prepared 13 formulations, such as percentage entrapment efficiency, percentage drug release, swelling index, percentage yield, and particle size analysis. The entrapment efficiency of optimized formulation was found to be 72.02%. The entrapment efficiency increases with increase in EC concentration and stirring speed. Optimized formulation was further subjected to study of drug release kinetics based on the R2 value; it was observed that Korsmeyer Peppas release kinetic model was found to be best suited for formulation of atenolol with EC: carbopol 934 by solvent evaporation method.
 Conclusion: The optimized formulation of microparticles containing atenolol was found to be homogeneous, good appearance and had well flow properties and better release kinetics.