Polyphenols found in fruits and vegetables are of great interest due to their health benefits. Gallic acid (GA) is an antioxidant with cytotoxic effects. Microspheres are drug carrier systems, where the active substance is trapped in matrix. A controlled release profile is aimed at the target region by preserving the loss of substance and activity. In this study, GA containing microspheres were formed with sodium alginate (NaAlg) in formulations with different ratios. The arrest efficiencies ranged between 11.26 and 72.64%. Release studies were performed at pH 7.4. Optimum conditions were determined as GA/NaAlg ratio 1/8. The microspheres were found to arrest GA and exhibit a controlled release profile. Microspheres were characterized by scanning electron microscope (SEM), differential scanning calorimetry (DSC), X-Ray diffraction (XRD), Fourier transform infrared spectrometer (FTIR) analysis. GA retained its antioxidant activity determined by DPPH (2,2-diphenyl-1-picrylhydrazyl) method and anticancer activity on Caco-2 cells. Further studies are necessary on GA-loaded NaAlg microspheres which have high potential to be used in adjunct and complementary therapies.