Enhanced Oral Bioavailability of Rivaroxaban-Loaded Microspheres by Optimizing the Polymer and Surfactant Based on Molecular Interaction Mechanisms

Abstract

This study aimed to develop microspheres using water-soluble carriers and surfactants to improve the solubility, dissolution, and oral bioavailability of rivaroxaban (RXB). RXB-loaded microspheres with optimal carrier (poly(vinylpyrrolidone) K30, PVP) and surfactant (sodium lauryl sulfate (SLS)) ratios were prepared. 1H NMR and Fourier transform infrared (FTIR) analyses showed that drug–excipient and excipient–excipient interactions affected RXB solubility, dissolution, and oral absorption. Therefore, molecular interactions between RXB, PVP, and SLS played an important role in improving RXB solubility, dissolution, and oral bioavailability. Formulations IV and VIII, containing optimized RXB/PVP/SLS ratios (1:0.25:2 and 1:1:2, w/w/w), had significantly improved solubility by approximately 160- and 86-fold, respectively, compared to RXB powder, with the final dissolution rates improved by approximately 4.5- and 3.4-fold, respectively, compared to those of RXB powder at 120 min. Moreover, the oral bioavailability of RXB was improved by 2.4- and 1.7-fold, respectively, compared to that of RXB powder. Formulation IV showed the highest improvement in oral bioavailability compared to RXB powder (AUC, 2400.8 ± 237.1 vs 1002.0 ± 82.3 h·ng/mL). Finally, the microspheres developed in this study successfully improved the solubility, dissolution rate, and bioavailability of RXB, suggesting that formulation optimization with the optimal drug-to-excipient ratio can lead to successful formulation development.

Bioavailability Enhancement Strategies for Rivaroxaban: A Noteworthy Review

“…These findings imply that optimizing the drug-to-excipient ratio can lead to successful formula development. Overall, the microspheres developed in this study successfully enhanced the solubility, dissolution rate, and bioavailability of RXB [11].…”

Novel Saccharomyces cerevisiae-Loaded Polyvinylpyrrolidone/SiO2 Nanofiber for Wound Dressing Prepared Using Electrospinning Method

“…Fourier transform infrared spectroscopy: FTIR patterns were obtained for samples in the range 4000–450 cm −1 using a PerkinElmer Frontier spectrometer (Waltham, MA, USA) [ 31 ].…”