Abstract Nanotechnology for oral cancer could be a use full tool for detection and drug therapy. By Possessing unprecedented potential for early stage detection, treatment of oral cancer, nanoparticles have been demonstrated over the last decade. In this review, we will summarize the current state-of-the-art of nanoparticles in biomedical applications such as detection, diagnosis and targeting over the oral cancer. Gold nanospheres, nanorods, nanoshells, nanocages, and surface enhanced nanoparticles will be discussed in detail regarding their uses in vivo imaging, cancer therapy, and drug delivery. The key feature of nanoparticle-based drug agents to target over ligands, therapeutic drugs, and other functionalities can all be integrated to allow for targeted molecular imaging and molecular therapy of oral cancer. The future of the nanotechnology for oral cancer looks brighter than ever yet many hurdles remain to be conquered. A multifunctional platform based on gold nanoparticles, with multiple receptor targeting, multimodality imaging, and multiple therapeutic entities, holds the promise for a “magic gold bullet” against oral cancer.