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Nanotechnology has recently gained promising advancements in the area of drug delivery. Nanocarriers have evolved for treating numerous disorders and show capability in delivering antitumor drugs at the targeted site. Due to enhanced biocompatibility and decreased toxicities, nanocarriers-based platforms permit the anticancer drug delivery into the tumors by disrupting the physiopathology of tumor endothelium by enhancing the healing efficiency for oncological ailments. Various nanocarriers, such as polymeric nanocarriers, dendrimers, micelles, carbon-based nanocarriers, nanocomposites, liposomes, and magnetic nanocarriers, show advanced efficacy in targeted drug delivery systems and improve the treatment efficacy. This chapter highlights the fabrication methods of various nanoparticles that are utilized as nanocarriers and their advanced results in targeted drug delivery systems.