Nanotechnology is a vital field in the physical, chemical, and medicinal arenas. It requires insight into the atomic and molecular structures of materials, so their relevance can be evaluated. Nanotechnology is like a sided sword in the field of medical care. It is beneficial in disease diagnosis, its treatment, reformative medicine, dentistry, gene therapy, cancer therapy, drug delivery, as well as in the aesthetics industry. Nanomaterials have unique morphology, can be used for safe and effective therapies, where drugs can be given productively with minimal side effects. Nanomaterial drug transporters assist the transfer of small molecules like proteins, nucleic acids and many more in the body. Nanotechnology helps to cure many chronic diseases by targeted delivery of the precise drug. Currently, nanomedicine has several applications, i.e. immunotherapeutic agents, chemotherapeutic agents, and biological agents, drug delivery, diagnostics and imaging (e.g. MRI, CT, PET scans), therapeutics, regenerative medicine, and surgical and monitoring applications, etc. This chapter highlights the multifaceted aspects of nanomaterials, corroborating their benefits for the healthcare industry. This chapter explores applications of nanomaterials in the delivery of drugs to targeted sites and improved diagnostic devices, and innovative advanced therapies in spite of perplexing pathophysiological conditions.