FORMULATION AND IN VITRO EVALUATION OF RIVAROXABAN MICROSPHERES

Abstract

Microsphere drug delivery methods have been utilized to boost effectiveness, reduce toxicity, and improve patient compliance. Additional benefits of using microspheres to deliver medications include controlled drug release, improved bioavailability, and targeted drug delivery to the desired location. In order to achieve the required therapeutic effect, Chitosan is encapsulated in a biodegradable microsphere delivery system and given orally. The benefit of microsphere formulations over traditional tablet or capsule formulations is that they increase the surface area exposed to the absorption site, boosting medication absorption and reducing drug dose frequency. An anticoagulant and the first orally active direct factor Xa inhibitor. Rivaroxaban microspheres were prepared by Ionotropic Gelation Technique using different ratios of Rivaroxaban and Sodium Alginate, along with polymers like HPMC K15M, Pectin and Chitosan. Rivaroxaban microspheres were evaluated for percentage yield, particle size. Surface morphology, flow properties, drug content and entrapment efficiency and were found to be within the acceptable range. Invitro dissolution studies of the microspheres revealed that the formulation F12 containing Chitosan as a polymer shows maximum drug release at the end of 12 hours, when compared with the other formulations. Drug release kinetics of the optimized formulation states that the formulation F12 follows zero order drug release with Super case II transport mechanism.