Extensive research and utilization of nanotechnology in cancer treatment have arisen because nanoparticles can serve as key agents for delivering drugs effectively. In contrast to traditional medications, utilizing nanoparticle-based drug delivery offers distinct benefits including enhanced stability and compatibility with biological systems, improved permeability and retention within the body, and particular directing capabilities. The advancement and utilization of hybrid nanoparticles, blending diverse nanoparticle characteristics, have propelled this form of drug carrier system to new heights. Cancer stands as a prominent contributor to both mortality and morbidity, characterized by a multifaceted pathophysiology. Conventional cancer treatments comprise chemotherapy, radiation therapy, targeted therapy, and immunotherapy. Nevertheless, challenges like non-specificity, cytotoxicity, and resistance to multiple drugs present significant obstacles for effective cancer therapy. Nanoparticles, ranging from 1 to 100 nm in size, offer unique advantages for cancer treatment, including biocompatibility, decreased toxicity, improved stability, enhanced permeability and retention, and accurate targeting. Furthermore, researchers have recently begun exploring the involvement of nanoparticles in immunotherapy, which holds increasingly significant promise in cancer treatment. This chapter examines various nanoparticle types, targeting strategies, and approved nanotherapeutics, focusing on their implications for cancer treatment. Additionally, we provide an overview of the present viewpoint, benefits, and obstacles in clinical application.