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Published on: March 1, 2024
Novel rivaroxaban-loaded microsphere systems with different surface microstructure for enhanced oral bioavailability
Min-Jong Choi1, Mi Ran Woo2, Kyungho Baek1
1Department of Pharmaceutical Engineering, Dankook University, 119 Dandae-Ro, Dongnam-Gu, Cheonan, 31116, South Korea.
This study developed three types of rivaroxaban-loaded polymeric microspheres. Solvent-evaporated microspheres significantly enhanced rivaroxaban
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Rivaroxaban is a widely used anticoagulant with poor aqueous solubility, limiting its oral bioavailability.
- Developing effective drug delivery systems is crucial for improving the therapeutic efficacy of poorly soluble drugs like rivaroxaban.
Purpose of the Study:
- To fabricate and compare three types of rivaroxaban-loaded polymeric microspheres with different surface microstructures.
- To evaluate the impact of these microspheres on the solubility, dissolution rate, and oral bioavailability of rivaroxaban.
Main Methods:
- Fabrication of rivaroxaban-loaded polymeric microspheres using spray-drying technique (solvent-evaporated, surface-attached, solvent-wetted).
- Characterization of microsphere physicochemical properties using SEM, XRD, DSC, and particle size analysis.
- In vitro evaluation of aqueous solubility and dissolution rate, followed by in vivo assessment of oral bioavailability in rats.
Main Results:
- Solvent-evaporated microspheres exhibited significantly higher aqueous solubility (approx. 208x) and dissolution rate (approx. 5x) compared to rivaroxaban powder.
- All three types of microspheres improved rivaroxaban's oral bioavailability, with solvent-evaporated microspheres showing the greatest increase (approx. 2x).
- The order of improvement in oral bioavailability was: solvent-evaporated > solvent-wetted > surface-attached microspheres.
Conclusions:
- Solvent-evaporated rivaroxaban-loaded polymeric microspheres represent a promising novel oral dosage form.
- This formulation strategy effectively enhances the oral bioavailability of poorly soluble rivaroxaban.
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