A Novel Approach for the Treatment of Hypertension: Gastroretentive Microballoons of Atenolol

Abstract

The formulation of atenolol-loaded microballoons involved the use of Eudragit RS 100, HPMC K4 M as a polymer, and span 80 as a surfactant. The microballoons were prepared by an emulsion solvent diffusion (non-aqueous) using liquid paraffin, methanol, and dichloromethane as a processing medium. The Box-Behnken design was utilized to get optimized formulation using a concentration of HPMC K4 M (A), Concentration of Eudragit RS 100 (B), Concentration of surfactant (C), and stirring speed (D) as an independent parameter while, Particle size (Y1), entrapment efficiency (Y2) and %buoyancy (Y3) using as a dependent parameter. For the optimised formulation, the mean particle size was 85.878 ± 1.063 μm, entrapment efficiency was 92.26 ± 1.65%, and buoyancy was 89.19 ± 1.48% found. An image of the formulation taken using a scanning electron microscope (SEM) reveals discrete particles with a smooth surface texture, a hollow interior, a spherical shape, and a particle size of less than 200 μm. The FTIR study confirms there was no interaction between the drug and excipients. The in-vitro drug release study found that atenolol-loaded microballoons released the drug for up to 12 hours as compared to the pure drug. This was due to increasing the gastric residence time and absorption area in the stomach. The drug release kinetic study reveals that it follows the Higuchi model and the drug release mechanism was type II transport which was obtained from the Korsmeyer Peppas model. The stability study shows that there is no significant change in the optimized microballoons for 30 days as per ICH guidelines.