This study aimed at improving the targeting and cytotoxic effect of ellagic acid (EA) on colon\ncancer cells. EA was encapsulated in chitosan (CHIT) polymers then coated by eudragit S100 (ES100)\nmicroparticles. The release of EAdouble-coatedmicroparticles (MPs) was tested at simulative pH values.\nMaximum release was observed at 24 h and pH7.4. The cytotoxicity of EAMPs onHCT 116 colon cancer\ncells was synergistically improved as compared with raw EA. Cell-cycle analysis by flow cytometry\nsuggested enhanced G2-M phase colon cancer cell accumulation. In addition, a significantly higher\ncell fraction was observed in the pre-G phase, which highlighted the enhancement of the proapoptotic\nactivity of EA formulated in the double-coat mixture. Annexin-V staining was used for substantiation\nof the observed cell-death-inducing activity. Cell fractions were significantly increased in early, late, and\ntotal cell death. This was backed by high elevation in cellular content of caspase 3. Effectiveness of the\ndouble-coated EA to target colonic tissues was confirmed using real-time iohexol dye X-ray radiography.\nIn conclusion, CHIT loaded with EA and coated with ES100 formula exhibits improved colon targeting\nas well as enhanced cytotoxic and proapoptotic activity against HCT 116 colon cancer when compared\nwith the administration of raw EA.
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