Cancer is a major global cause of death that requires new approaches to treatment outside the use of traditional chemotherapy, radiotherapy, and surgery. Nanomedicine, based on the application of nanoparticles (NPs) to targeted drug delivery, offers an exciting area of research for increased therapeutic benefits while reducing side effects. In this review, developments in nanotechnology-based drug delivery systems (DDSs) are discussed, focusing on their value in transcending multidrug resistance (MDR), improving bioavailability, and increasing the specificity of treatment. Several NP-based systems, such as liposomes, polymeric NPs, metal NPs, and quantum dots, are analyzed with respect to cancer therapy. Additionally, this paper addresses issues with clinical translation, including biocompatibility, toxicity, and regulatory issues. At last, upcoming trends and directions of future studies to optimize NP-based cancer treatments are presented.