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In this chapter, an overview of the progress made in the application of nanoparticles in the treatment of liver cancer by drug delivery is provided. Nanotechnology has had an important role in the development of delivery vectors so far. Due to the remarkable properties of nanoparticles, they have long been considered as a potential tool for the diagnosis of various cancers and for drug delivery applications. These properties include high surface area to volume ratio, surface plasmon resonance, surface chemistry and multifunctionalization, facile synthesis, and a stable nature. This chapter summarizes current nanovectors for small interfering RNA (siRNA) delivery, and a multistage vector system for tumor-specific delivery. The design of siRNA therapeutics and their mechanism of action in terms of cancer cell killing, including effective delivery of therapeutics in vivo are considered. Moreover, the nontoxic and nonimmunogenic nature of gold nanoparticles and the application of gold nanoparticles in the treatment of cancer by tumor detection and drug delivery are presented.