Potential applications of gold nanoparticles in biomedicine have increasingly been reported on account of the ease of synthesis, bioinert characteristics, optical properties, chemical stability, high biocompatibility, and specificity. The safety of these particles remains a great concern, as there are differences among toxicity study protocols used. This article focuses on integrating results of research on the toxicological behavior of gold nanoparticles. This can be influenced by the physicochemical properties, including size, shape, surface charge, and other factors, such as methods used in the synthesis of gold nanoparticles, models used, dose, in vivo route of administration, and interference of gold nanoparticles with in vitro toxicity assay systems. Several researchers have reported toxicological studies with regard to gold nanoparticles, using various in vitro, in vivo, and in ovo models. The conflicting results concerning the toxicity of gold nanoparticles should thus be addressed to justify the safe use of gold nanoparticles in biomedicine.