Thermal sintering driven modulation of drug release and buoyancy characteristics in dasatinib gastro-retentive tablets

Abstract

Background: Thermal sintering is emerging as an innovative and cost-effective technique in pharmaceutical formulation design, especially for controlling drug release in oral dosage forms. This study investigates its applicability in the development of gastro-retentive floating tablets for Dasatinib, a tyrosine kinase inhibitor with low solubility and bioavailability. Methodology: Floating matrix tablets were developed via direct compression, incorporating carnauba wax and hydroxypropyl methylcellulose as matrix-forming agents, along with sodium bicarbonate as a gas-generating component to impart buoyancy. The tablets were then thermal-sintered at two temperatures for varying durations in a controlled hot-air oven. The effects of thermal sintering conditions were investigated with respect to in vitro dissolution, mechanical strength, percent water uptake, percent erosion, total buoyancy duration, floating lag time, and SEM morphology. Results and Discussion: Statistical analysis using two-way ANOVA (α = 0.05) revealed that sintering condition significantly influenced drug release and buoyancy performance (p < 0.01). Formulation DST 02 sintered at 70°C-3 hours exhibited optimal performance, achieving a maximum drug release of 96.3% over 13 hours. Characterization technique methods such as FTIR and DSC have confirmed the absence of chemical interactions and polymorphic transitions. Stability studies conducted in accordance with ICH guidelines indicated that the optimized formulation remained stable throughout the study period. Conclusion: Thermal sintering effectively modulated the release characteristics of Dasatinib from floating tablets, thereby increasing gastric retention time and facilitating sustained drug release. This technique holds promise for improving therapeutic efficacy, reducing dosing frequency, and enhancing patient compliance in oral drug delivery.