The rapid emergence of gold nanoparticles (AuNPs) technology holds great promise for future applications due to their large volume specific surface areas with high diverse surface activities than bulk gold. These properties have made AuNPs of great importance in the development of excellent nanoelectronic chips, promising vehicle for a wide range of biomedical and environmental applications. However, the huge impact arising from the physiochemical properties has given rise to new concerns for future health status. Currently, there is dearth information on AuNPs health effects and no regulatory safety and guidelines relating their properties to toxicities. This review, therefore, focuses on the potential toxicological aspect of AuNPs experienced so far and their interactions with biological systems. These can be applied as measures to improve their biomedical applications and risk assessment. However, assessing the safety issues of nanoparticles is quite challenging, because of the vast physiochemical properties that confound their biomedical and toxicological profiles. Therefore more research with standardized NPs physicochemical properties is needed based on the different types of AuNPs to establish both in vitro and in vivo nanotoxicities. The establishment of each size with specific ligand properties will update the complex conflicting ideas emanating from the different AuNPs safety studies thereof.