The development of nanocarriers for targeted drug delivery has advanced significantly in the field of nanomedicine recently, and they assure to enhance efficacy and reducing side effects related to traditional chemotherapy. Gold, magnetic, polymeric, carbon-based, and silver nanoparticles are most commonly used as nanocarriers for chemotherapy. They exhibit different properties according to their shape, size and surface functionality for specific applications. These nanocarriers have wide the range of applications including targeted drug delivery, CNS drug delivery, pharmaceutical industry, tissue regeneration and gene therapy. Although they have some challenges and limitations, ongoing research hopes to eradicate them. This chapter presents a summary of mechanism, design and characterization, toxicity, applications and future advancement of nanocarriers in targeted drug delivery and chemotherapy.