Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats.

摘要: Olmesartan medoxomil (OM) is hydrolyzed to its active metabolite olmesartan by the action of aryl esterase exert antihypertensive actions selectively blocking angiotensin II-AT1 receptor. Poor aqueous solubility and uncontrolled enzymatic conversion OM poorly permeable limits oral bioavailability. The aim current study was formulate a novel nanoemulsion improve pharmacokinetics therapeutic efficacy. oil-in-water (o/w) developed using lipoid purified soybean oil 700, sefsol 218 solutol HS 15. We have characterized nanoemulsions considering their thermodynamic stability, morphology, droplet size, zeta potential viscosity in vitro drug release characteristics fasting state simulated gastric fluid (pH 1.2) intestinal 6.5). thermodynamically stable comprises spherical nanometer sized droplets (<50 nm) with low polydispersity index showed enhanced permeability through Caco-2 cell monolayer. concentration rat plasma following absorption determined our validated LC-MS/MS method. result pharmacokinetic 2.8-fold increased area under curve (AUC0-27) upon administration sustained profile. Subsequent, vivo studies demonstrated better prolonged control experimentally induced hypertension 3-fold reduction conventional dose. By analysing findings present investigations based on stability study, permeability, profile pharmacodynamic evaluation indicated that (OMF6) could significantly enhance bioavailability relatively insoluble contributing improved clinical application.