In the last years, biomedical research has focused its efforts in the development of new oral delivery systems for the treatment of different diseases. Ferulated arabinoxylans are polysaccharides from cereals that have been gaining attention in the pharmaceutical field due to their prebiotic, antioxidant, and anticancer properties. The antioxidant and anticancer properties of these polysaccharides make them attractive compounds for the treatment of cancer, particularly colon cancer. In addition, ferulated arabinoxylans can form covalent gels through the cross-linking of their ferulic acids. Due to their particular characteristics, ferulated arabinoxylan gels represent an excellent alternative as colon-targeted drug delivery systems. The aim of the present work is to review the physicochemical and functional properties of ferulated arabinoxylans and their gels and to present the future perspectives for potential application as antioxidant and anticancer agents.