ABSTRACT

Gastric cancer is a leading disease for considerable death across the globe and the research aimed to treat it with improved patient compliance and bioavailability by targeting the stomach as a site of action. Trifluridine-Tipiracil (TFD–TPI) is a fixed-dose medication combined with two active pharmaceutical ingredients. TPI increases the bioavailability of TFD by preventing the rapid metabolism of TFD. The drawback of shorter biological half-life and low bioavailability of TFD can be resolved by combining it with TPI in floating microspheres which releases the drug for an extended period in the stomach with better patient compliance. TPI-TFD floating microspheres are prepared by water-in-oil-in-oil (W/O1/O2) double emulsion solvent diffusion method using ethyl cellulose, and hydroxy propyl methyl cellulose. The polymer ratio, rotational speed and solvent volume are optimised by Box Behnken design. The percentage entrapment efficiency (Y1), Time required for 50% drug release (Y2) and particle size (Y3) were taken as dependent variables. The % EE of the optimised batch was 76.5 and 77%, T50% was 5.39 and 5.06 hours, particle size was 300 ?m and the % drug release was 100.30 %. A kinetic study of in vitro drug released by anomalous diffusion. The FT-IR and DSC analysis confirmed compatibility between drug and excipients in spherical-shaped microspheres. Gas chromatography reveals that the trace amount of residual solvents was within accepted limits. The average sizes of spherical-shaped microspheres were found to have a thickness of 303 nm. The optimised batch (B-13) was subjected to a short-term stability study per ICH guidelines indicating no significant changes in evaluation criteria at 40°C/75% RH after 6 months. The MTT assay using AGS gastric cancer cell lines shows TFD-TP-loaded microspheres inhibited AGS cell growth. The findings demonstrate that the developed floating microspheres would provide stomach-specific controlled drug release for 12 hours with improved bioavailability to treat gastric cancer. Keywords: Gastric cancer, Box Behnken Design, floating microsphere, In v?tro cytotoxicity- study, Trifluridine, Tipiracil HCl
Publication date: 01/01/2026

https://ijbpas.com/pdf/2026/January/MS_IJBPAS_2026_9790.pdf

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https://doi.org/10.31032/IJBPAS/2026/15.1.9790