Novel rivaroxaban‑loaded microsphere systems with different surface microstructure for enhanced oral bioavailability
- Title
- Novel rivaroxaban‑loaded microsphere systems with different surface microstructure for enhanced oral bioavailability
- Author
- 최한곤
- Keywords
- Rivaroxaban; Polymeric microsphere; Microenvironment; Solubility; Oral bioavailability
- Issue Date
- 2023-09-04
- Publisher
- SPRINGER HEIDELBERG
- Citation
- DRUG DELIVERY AND TRANSLATIONAL RESEARCH
- Abstract
- This study compares rivaroxaban-loaded polymeric microsphere systems with three types of surface microstructure. Three
types of polymeric microspheres loaded with rivaroxaban were fabricated using a spray-drying technique: solvent-evaporated,
surface-attached, and solvent-wet microspheres, depending on whether the drug and additives used are soluble in the solvent.
The solvent-evaporated and surface-attached microspheres had a rivaroxaban/polyvinylpyrrolidone/sodium lauryl sulfate (SLS)
weight ratio of 1/0.25/2.2, and the solvent-wetted microspheres contained rivaroxaban/polyvinyl alcohol/SLS in equal weight
ratio (1/0.25/2). The physicochemical properties of the microspheres were evaluated using scanning electron microscopy,
powder X-ray diffraction, differential scanning calorimetry, and particle size distribution analysis. The aqueous solubility and
dissolution rate of rivaroxaban in the three types of microspheres were compared to those of the drug powder. The solvent evaporated, surface-attached, and solvent-wetted microspheres were approximately 208, 140, and 172 times as soluble as the drug powder, and the final dissolution rate (120 min) was approximately 5, 2, and 4 times that of the drug powder, respectively. In addition, the oral bioavailability increased by approximately 2, 1.3, and 1.6 times compared to that of the drug powder (area under drug concentration–time curve: 2101.3±314.8, 1325.2±333.3, and 1664.0±102.6 h·ng/mL, respectively). Finally, the solvent-evaporated microspheres showed the greatest improvement (solvent evaporating microspheres>solvent wetted microspheres>surface-attached microspheres≥drug powder). Therefore, the solvent-evaporated microspheres may represent a novel oral dosage form that improves the oral bioavailability of rivaroxaban, a poorly soluble drug.
- URI
- https://link.springer.com/article/10.1007/s13346-023-01420-whttps://repository.hanyang.ac.kr/handle/20.500.11754/188099
- ISSN
- 2190-3948
- DOI
- 10.1007/s13346-023-01420-w
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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