Among the several types of nanoparticles in existence, anisotropic gold-based nanoparticles demonstrate special advantages because of their unique properties. Gold nanoparticles can be prepared and modified with a wide range of functional materials including polymers, surfactants, ligands, dendrimers, drugs, DNA, RNA, proteins, peptides, and oligonucleotides. Hence, they are a promising vehicle for bioimaging, drug delivery, and other therapies. This review mainly addresses the properties, preparation, and applications of anisotropic gold nanoparticles in biomedical applications and targeted drug delivery.