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KMID : 1146920200500040399
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Journal of Pharmaceutical Investigation
2020 Volume.50 No. 4 p.399 ~ p.411
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Febuxostat loaded β-cyclodextrin based nanosponge tablet: an in vitro and in vivo evaluation
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Amin Omnya M.
Ammar Amal
Eladawy Shereen A.
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Abstract
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Purpose: Febuxostat is non-purine, selective inhibitor of xanthine oxidase for treatment of gout. It exhibits poor bioavailability. The goal of the present study was to enhance the oral bioavailability of Febuxostat through β-Cyclodextrin nanosponges, subsequently reduce the dose and side effects.
Methods: Nanosponges were formed by cross-linking β-Cyclodextrin with carbonate bonds using different molar ratio (1:4, 1:6, 1:8 and 1:10 β-Cyclodextrin: crosslinker). Drug was incorporated by solvent evaporation method. Nanosponge formulations were evaluated and formulations that released (≥?30%) at first hour followed by controlling the release (≥?75%) at 6 h were further evaluated and tableted by direct compression. The optimum tablet formulations based upon drug release were investigated for accelerated stability testing and for comparative bioavailability with a marketed product.
Results: SEM illustrates porous and sponge like structure. DSC and FTIR studies confirmed the formation of nanosponges and encapsulation of Febuxostat within it. The zeta-potentials were high (??21.5 to ??32.3 mV). The particle sizes were between 224.7 and 305.6 nm. The in vitro release study showed a biphasic release pattern. Oral bioavailability of selected formulation and marketed product showed enhanced Cmax (1655.0?±?18.5 vs. 1592.7?±?95.9 ng/mL) and AUC0?∞ (14,576.7?±?1681.7 vs. 6449.7?±?677.1 ng h/mL). The relative bioavailability was found to be 217.9%.
Conclusion: Nanosponges is a feasible approach to improve the oral bioavailability of Febuxostat.
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KEYWORD
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β-Cyclodextrin, Diphenyl carbonate, Febuxostat, Gout, Nanosponges
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