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Nanotechnology refers to research and technology development at the nanoscale. Objects at this scale, such as “nanoparticles,” take on novel properties and functions that differ markedly from those seen in the bulk scale. The small size, improved solubility, large surface to mass ratio and multifunctionality of nanoparticles open many new research vistas for biologists. The novel properties make these materials superior; crucial in many areas of human activity. This rapidly growing field allows cross-disciplinary researchers the opportunity to design and develop multifunctional nanoparticles that can target, diagnose, and treat diseases such as cancer. Current modalities of treatment and diagnosis of various diseases, especially cancer have major limitations such as drug resistance or drug toxicities and poor sensitivity or specificity respectively. Newer and improved methods of cancer detection and treatment based on nanoparticles are being developed. In this review, a brief sketch of various kinds of nanomaterials and their role in molecular diagnosis, drug targeting, and development of nanomedicine is discussed.