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Current Drug Therapy

Author(s): Ravina Kathota, Chetna Modi*, Vaishali Thakkar, Hardik Rana and Ayushi Patel

DOI: 10.2174/1574885518666230331084428

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Development and Characterization of Febuxostat Loaded Floating Beads as Gastro-retentive Drug Delivery System in the Treatment of Gout: A Statistical Approach

Page: [433 - 444] Pages: 12

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Abstract

Background: Febuxostat is a BCS class-II drug, used in the treatment of gout. However, because of its lower solubility, a higher and more frequent dose of the drug is required in the treatment.

Objective: The objective of this research was to develop and evaluate febuxostat-loaded floating beads as a gastro-retentive drug delivery system (GRDDS) to target drug release up to 24hr in order to enhance bioavailability.

Methodology: Gastro-retentive floating beads were formulated using the ionotropic gelation method. Screening of lipids was carried out based on the shape and texture of floating beads. Drug-excipient compatibility study was done using DSC analysis. Further optimization of gastro-retentive floating beads of febuxostat was performed by Box-Behnken design using gelucire 43/01, lactose, and soluplus as independent variables and %drug entrapment and %drug release after 24 hr as dependent variables. Evaluation of the optimized batch was performed for in vitro buoyancy, %drug entrapment, %drug release, FTIR, and SEM study.

Result and Discussion: In the ANOVA, contour plots, and 3D surface plots, the optimized batch showed 93.95±0.29 % drug entrapment and 88.14±0.58 % drug release after 24 hr with 98%±1% invitro buoyancy. Overlay plots and checkpoint batches were accompanied to confirm the optimization. Polynomial equations proved the positive effect of lipids on drug entrapment and drug release. SEM images explained porous and microstructures on beads.

Conclusion: In conclusion, gastro-retentive febuxostat floating beads were successfully developed and characterized for once a daily dose with enhanced bioavailability and reduced cost of therapy.

Graphical Abstract

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