MICROSPHERE-BASED DELIVERY OF DABIGATRAN: ADVANCES IN CONTROLLED RELEASE ANTICOAGULANT THERAPY

Dabigatran etexilate, a direct thrombin inhibitor, has emerged as a valuable oral anticoagulant for the prevention and treatment of thromboembolic disorders. Despite its clinical utility, conventional formulations of dabigatran are limited by low oral bioavailability, dependence on intestinal transporters, and variability in patient response. These challenges have stimulated interest in advanced drug delivery systems, particularly microsphere-based formulations, to optimize therapeutic outcomes. Microspheres, prepared using techniques such as ionic gelation, emulsion coacervation, solvent evaporation, and spray drying, encapsulate dabigatran within biodegradable polymers including chitosan, Eudragit RL100, and PLGA. Such systems offer controlled and sustained drug release, enhanced gastrointestinal stability, and improved absorption, thereby addressing the pharmacokinetic shortcomings of conventional tablets. By maintaining steady plasma concentrations and reducing peak–trough fluctuations, microsphere formulations improve pharmacodynamic predictability, minimize bleeding risks, and enhance patient compliance through reduced dosing frequency. This review highlights the formulation strategies, polymeric approaches, and pharmacokinetic improvements achieved with dabigatran microspheres, while also discussing their translational potential and future directions. Microsphere-based delivery represents a promising advancement in controlled release anticoagulant therapy, with the potential to transform clinical practice by offering safer, more effective, and patient-friendly treatment options. KEYWORDS: Dabigatran etexilate, Microspheres, Controlled release drug delivery, anticoagulants, Bioavailability, Thrombin