Design, Development, and Assessment of Gastro-Retentive Drug Delivery System for the Management of Hypertension

Abstract

For the effective management of hypertension, we have developed a gastro-retentive drug delivery system that includes simvastatin and candesartan. Candesartan, a synthetic angiotensin II receptor antagonist made from benzimidazole, is a prodrug with antihypertensive properties. The medication simvastatin belongs to the pharmacological family of HMG-CoA reductase inhibitors. This lowers blood levels of harmful cholesterol, including low-density lipoprotein (LDL), and triglycerides. To achieve the optimal therapeutic medicine level over a long period of time, a controlled release mechanism was developed in the form of floating microspheres. Using the emulsion solvent evaporation technique with different quantities of ethyl cellulose, HPMC, and chitosan, floating microspheres carrying simvastatin and candesartan were produced. For each formulation, three batches were made in order to evaluate repeatability with regard to percentage yield, entrapment efficiency, particle size, percentage buoyancy, and percentage drug release. The average particle size for simvastatin and candesartan was found to be between 49.94 and 93.1 µm and 65.66 and 105.28 m, respectively. For candesartan and simvastatin, the percentage drug loading efficiency of microspheres ranged from 58.36 to 93.08% and 54.85 to 83.64 percent, respectively. The percentage yield of microspheres for simvastatin and candesartan for all formulations varied from 56.32% to 78.65% and 43.68% to 98.32%, respectively. The optimised buoyancy of the candesartan and simvastatin microspheres was 80.63 and 89.98 percent, respectively. Simvastatin microspheres demonstrated a 64.35 percent release after 12 hours, but the optimised formulation of candesartan and Simvastatin demonstrated a sustained release of the medicine, releasing 62.34% of the drug until the 12-hour mark.