Key result
Rivaroxaban-loaded nanoparticles demonstrated sustained drug release (28.34% at 72 h), expressive time-dependent anticoagulant activity in vitro, and a non-toxic profile.
Why the study?
Rivaroxaban causes adverse effects primarily due to pharmacokinetic limitations, highlighting the need for more effective formulations.
Rivaroxaban-loaded PLGA/poloxamer nanoparticles demonstrate sustained drug release, effective anticoagulant activity in vitro, and a non-toxic profile, suggesting potential for developing new therapies for thrombotic disorders.
Answers are grounded in this paper and cite their sources.
Nanoparticle rivaroxaban shows sustained in vitro release and safety; leaves open clinical translation from animal data.
Rivaroxaban (RXB), an oral direct factor Xa inhibitor, presents innovative therapeutic profile. However, RXB has shown adverse effects, mainly due to pharmacokinetic limitations, highlighting the importance of developing more effective formulations. Therefore, this work aims at the preparation, physicochemical characterization and in vitro evaluation of time-dependent anticoagulant activity and toxicology profile of RXB-loaded poly(lactic-co-glycolic acid) (PLGA)/poloxamer nanoparticles (RXBNps). RXBNp were produced by nanoprecipitation method and physicochemical characteristics were evaluated. In vitro analysis of time-dependent anticoagulant activity was performed by prothrombin time test and toxicological profile was assessed by hemolysis and MTT reduction assays. The developed RXBNp present spherical morphology with average diameter of 205.5 ± 16.95 nm (PdI 0.096 ± 0.04), negative zeta potential (-26.28 ± 0.77 mV), entrapment efficiency of 91.35 ± 2.40%, yield of 41.81 ± 1.68% and 3.72 ± 0.07% of drug loading. Drug release was characterized by an initial fast release followed by a sustained release with 28.34 ± 2.82% of RXB available in 72 h. RXBNp showed an expressive time-dependent anticoagulant activity in human and rat blood plasma and non-toxic profile. Based on the results presented, it is possible to consider that RXBNp may be able to assist in the development of promising new therapies for treatment of thrombotic disorders.
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Machado et al. (2020) studied Thrombotic disorders. Rivaroxaban-loaded poly(lactic-co-glycolic acid) (PLGA)/poloxamer nanoparticles (RXBNps) was evaluated on Time-dependent anticoagulant activity and toxicological profile. Rivaroxaban-loaded nanoparticles demonstrated sustained drug release (28.34% at 72 h), expressive time-dependent anticoagulant activity in vitro, and a non-toxic profile.
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