Formulation And Evaluvation of Metoprolol Succinate Microspheres for The Management of Angina Pectoris

Angina pectoris, characterized by chest pain, arises from inadequate blood flow to the heart muscle, disrupting the delicate balance between oxygen supply and demand, ultimately resulting in reduced blood flow to the heart.This research focuses on developing and evaluating mucoadhesive microspheres containing Metoprolol succinate, a cardio selective beta-blocker, for managing angina pectoris, hypertension, heart attacks, and arrhythmias. A drug with a short half-life (4-6 hours) was formulated into microspheres using the ionic gelation method. To optimize the formulation, a Box-Behnken design (BBD) was applied, considering three independent factors: Carbopol 934P (X1) amount of Eudragit RL 100 (X2) and stirring speed (RPM) (X3). The optimized formulation was evaluated based on four dependent variables were particle size (Y1), entrapment efficiency (Y2), cumulative drug release (CDR) in 3 hours (Y3), and total drug release in 12 hours (Y4). A total of 17 formulations were tested, with all characterization tests performed in triplicate to ensure accuracy.To assess optimization data, response variables were evaluated. Formulated microspheres underwent Scanning Electron Microscopy (SEM), micrometric analysis, entrapment efficiency, and in vitro mucoadhesion and drug release studies. Response surface graphs and contour plots helped understand factor-level effects. Optimized formulation F11 (1250mg X1, 500mg X2, 1000rpm X3) showed close agreement between predicted and experimental values. F11 demonstrated 83.14% entrapment efficiency and a particle size of 149.6μm.A cumulative drug release of 9.89% was observed within 3 hours, followed by a controlled release of 94.4% over 12 hours. The study revealed that polymer concentration significantly impacted the release profile. By optimizing polymer concentration and stirring speed, metoprolol succinate microspheres can be effectively formulated to achieve desired controlled release characteristics, offering a promising treatment for angina pectoris.