Ibuprofen (IBU) is one of the most-sold anti-inflammatory drugs in the world, and its residues can reach aquatic systems, causing serious health and environmental problems. Strategies are used to improve the photocatalytic activity of zinc oxide (ZnO), and thosethat involvethe inclusion of metalhave received special attention. The aim of this work was to investigate the influence of the parameters and toxicity of a photoproduct using zinc oxide that contains cerium (ZnO-Ce) for the photodegradation of ibuprofen. The parameters include the influence of the photocatalyst concentration (0.5, 0.5, and 1.5 g L−1) as well as the effects of pH (3, 7, and 10), the effect of H2O2, and radical scavengers. The photocatalyst was characterized by Scanning Electron Microscopy-Energy Dispersive Spectroscopy, Transmission electron microscopy, Raman, X-Ray Diffraction, surface area, and diffuse reflectance. The photocatalytic activity of ibuprofen was evaluated in an aqueous solution under UV light for 120 min. The structural characterization by XRD and SEM elucidated the fact that the nanoparticle ZnO contained cerium. The band gap value was 3.31 eV. The best experimental conditions for the photodegradation of IBU were 60% obtained in an acidic condition using 0.50 g L−1 of ZnO-Ce in a solution of 20 ppm of IBU. The presence of hydrogen peroxide favored the photocatalysis process. ZnO-Ce exhibited good IBU degradation activity even after three photocatalytic cycles under UV light. The hole plays akey role in the degradation process of ibuprofen. The toxicity of photolyzed products was monitored against Artemia salina (bioindicator) and did not generate toxic metabolites. Therefore, this work provides a strategic design to improve ZnO-Ce photocatalysts for environmental remediation.