Nanomaterials are popularly used in drug delivery, disease diagnosis and therapy. Among a number of functionalized nanomaterials such as carbon nanotubes, peptide nanostructures, liposomes and polymers, gold nanoparticles (Au NPs) make excellent drug and anticancer agent carriers in biomedical and cancer therapy application. Recent advances of synthetic technique improved the surface coating of Au NPs with accurate control of particle size, shape and surface chemistry. These make the gold nanomaterials a much easier and safer cancer agent and drug to be applied to the patient’s tumor. Although many studies on Au NPs have been published, more results are in the pipeline due to the rapid development of nanotechnology. The purpose of this review is to assess how the novel nanomaterials fabricated by Au NPs can impact biomedical applications such as drug delivery and cancer therapy. Moreover, this review explores the viability, property and cytotoxicity of various Au NPs.