Experimental design, formulation, and <i>in-vivo</i> evaluation of novel anticoagulant Rivaroxaban loaded cubosomes in rats model

Hashemy, Hadeer A. El-; Salama, Abeer; Rashad, Amira

doi:10.1080/08982104.2022.2153137

Cited by 2 publications

(2 citation statements)

References 28 publications

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“…Bioavailability refers to the amount of a drug that is absorbed into the bloodstream and is available to exert its therapeutic effect. For RXB, bioavailability is affected by several factors, including the route of administration, food intake, and drug interactions [5,7].…”

Section: Fig 1: Rivaroxaban Structurementioning

confidence: 99%

“…Since then, the drug has been approved for use in a variety of other medical settings, including the treatment of deep vein thrombosis and pulmonary embolism. Recently, RXB has been used to prevent disease progression in hospitalized patients with Coronavirus disease (Covid- 19), as well as to prevent thrombosis in non-valvular atrial fibrillation (NVAF) patients and obese patients [5,6].…”

Section: Introductionmentioning

confidence: 99%

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Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

AL-SHOUBKI,

H. TEAIMA,

ABDELMONEM

et al. 2023

Int J App Pharm

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This review article discusses Rivaroxaban (RXB), an anticoagulant that has gained much attention due to its ability to prevent blood clots from forming in the body. However, one of the major challenges pharmaceutical companies face is the low water solubility of RXB, which can lead to difficulties in formulating the drug for oral administration and affect the drug's bioavailability. However, to the best of our knowledge, limited studies have explored enhancing the bioavailability of the RXB. Most of these studies have been purely academic and impractical for industrial use. Therefore, this review article aims to discuss successful studies that have increased the bioavailability of RXB. The goal is to inspire researchers to develop this new drug further. The article covers seven strategies for enhancing the bioavailability of RXB, including microspheres, liposomes, self-nano emulsifying drug delivery system, solid lipid nanoparticles, cocrystals, sustained release, and solid dispersion. The studies discussed in this review offer valuable insights into developing novel drug delivery systems that can help overcome the limitations of existing drugs.

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Section: Fig 1: Rivaroxaban Structurementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

AL-SHOUBKI,

H. TEAIMA,

ABDELMONEM

et al. 2023

Int J App Pharm

View full text Add to dashboard Cite

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

Faheim,

Maghraby,

Sultan

2024

AAPS PharmSciTech

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Rivaroxaban is an anticoagulant for avoidance and therapy of thromboembolic disorders. Unfortunately, oral bioavailability of rivaroxaban is compromised with dose increments. Accordingly, the aim was to test nano-vesicular lipid systems for improved oral anticoagulation activity of rivaroxaban. Rivaroxaban loaded niosomes, bilosomes and spanlastic formulations were prepared. The prepared systems were assessed in terms of particle size, zeta potential, transition electron microscopic features (TEM), entrapment efficiency, in-vitro drug release, and in-vivo anticoagulation performance in rats. The prepared vesicular systems exposed spherical negatively charged vesicles with mean particle size values between 136.6 nm to 387.9 nm depending on the composition. Rivaroxaban was efficiently entrapped in the vesicular systems with entrapment efficiency values ranging from 92.4% to 94.0%. Rivaroxaban underwent sustained release from the fabricated vesicular systems. The in vivo performance of the tested preparation revealed significant enhancement of the anticoagulation parameters. This was manifested from the prolonged clotting time, and prothrombin time. Moreover, the cut tails of the examined rats receiving the formulated nano-systems exposed a lengthy tail bleeding time compared to those receiving the un-processed rivaroxaban aqueous dispersion. In Conclusion, niosomes, bilosomes and spanlastic nano-dispersions have a potential to overwhelm the oral anticoagulation efficiency of rivaroxaban with spanlastic ranked as best. Graphical Abstract

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Experimental design, formulation, and in-vivo evaluation of novel anticoagulant Rivaroxaban loaded cubosomes in rats model

Cited by 2 publications

References 28 publications

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

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

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