Phytochemicals as dietary constituents are being widely explored for the prevention and treatment of various diseases. Quercetin, a major constituent of various dietary products, has attracted extensive interest due to its anti-proliferative capability, reversal of multidrug resistance, autophagy promotion and tumor microenvironment modulation on different cancer types. Although quercetin has shown potent medical value, its application as an antitumor drug is limited. Problems like poor solubility, bioavailability and stability, short half-life and weak tumor-targeting biodistribution make quercetin an unreliable candidate for cancer therapy. Nanoparticle based platforms have shown a number of advantages in delivering a hydrophobic drug like quercetin to diseased tissues. Quercetin nanoparticles have demonstrated high encapsulation efficiency, stability, sustained release, prolonged circulation time, improved accumulation at tumor sites and therapeutic efficiency. Moreover, a combination of quercetin with other diagnostic or therapeutic agents in one nanocarrier has achieved enhancements in detecting or treating tumors. In this review, we have tried to summarize the pharmacological activities of quercetin with regard to tumor cells and microenvironments in vitro and in vivo. Furthermore, various nanoformulations have been highlighted for quercetin delivery for cancer treatment. These results suggest that quercetin nanoparticles may be a promising antitumor therapeutic agent.