Vesicular Carriers for Improved Oral Anticoagulation Competence of Rivaroxaban: In Vitro and In Vivo Investigation

    November 2024 in “ AAPS PharmSciTech ”
    Samar H. Faheim, Gamal M. El Maghraby, Amal A. Sultan
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    Studysummary In this study, researchers found that niosomes, bilosomes, and spanlastic formulations can enhance the oral anticoagulation efficiency of rivaroxaban in rats, with spanlastic ranked as the most effective in prolonging clotting, prothrombin, and tail bleeding times compared to unprocessed rivaroxaban.
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    The study investigated the use of nano-vesicular lipid systems to improve the oral anticoagulation activity of rivaroxaban, an anticoagulant with compromised bioavailability at higher doses. Rivaroxaban was loaded into niosomes, bilosomes, and spanlastic formulations, which were evaluated for particle size, zeta potential, entrapment efficiency, and drug release. The vesicular systems showed spherical, negatively charged vesicles with particle sizes from 136.6 nm to 387.9 nm and high entrapment efficiency (92.4% to 94.0%). In vivo tests in rats demonstrated enhanced anticoagulation, with prolonged clotting and prothrombin times, and increased tail bleeding time compared to unprocessed rivaroxaban. Spanlastic formulations were identified as the most effective in improving rivaroxaban's oral anticoagulation efficiency.
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