“Nanotechnology in Drug Discovery and Delivery” was coined to explain how nanotechnology will be used in biomedical sciences due to the tiny functional elements of living cells. Nanotechnology has strengthened biological-physical links by using nanostructures and nanophases in many study domains. Nanotechnology develops materials, devices, and systems by controlling matter at the nanoscale, or atomic and molecular level. Nanotechnology can create targeted and site-specific nanoparticles that deliver medications to any harmful molecular target in the body. Biomedical sciences and nanotechnology produce great stability, binding, bioavailability, biodistribution, and enzymatic drug breakdown resistance. Nanomaterials are 1–100 nm in size. Material size affects tissue engineering, drug delivery, biosensors, microfluidics, and microarray tests in nanomedicine. Engineered nanoparticles could greatly improve illness diagnosis and treatment. Nanotechnology can help overcome classical delivery constraints, such as biodistribution and intracellular trafficking, by targeting cells, transporting molecules to organelles, and other methods. It aids drug discovery, nanocarrier drug delivery, implants, therapeutic nanomaterials, and tiny device and sensor applications. This chapter discusses biocompatible nanomaterials such as liposomes, biopolymer/polymeric nanoparticles, dendrimers, quantum dots (QDs), metallic nanoparticles, nanocrystals, and nanoalloys for medical implants. To provide a broad perspective, impediments, challenges, and future potential have been discussed in addition to nanoparticle therapeutic uses. The chapter concludes that nanomaterials can be used in biomedical research for drug delivery, discovery, and diagnostics.