Nanobiotechnology is a multi-strategic approach that engineers biological components (atoms and molecules) at the nanoscales. The concept was introduced as an effective alternative with drug delivery and targeting properties. Nanobiotechnology has several applications in cancerous disease, autoimmune, inflammation, infectious, and viral diseases, and for the management of COVID-19. Nanoparticles have biomimetic properties, encapsulation, and safety formulation of drugs, and all these properties give them an advantage over conventional drug strategies. Nanobiotechnology research is currently progressive and needs extensive exploration and understanding for its potential use in future innovations. The present review studied the concept of nanobiotechnology, its origin, mechanism of drug delivery and targeting, applications, and future perspective in pharmacology and innovation to decipher its role in future advanced research.