Chemoprevention through the use of bioactive food components is a practical approach for cancer control. Despite abundant efficacy data under preclinical settings, this strategy has resulted in limited success for human cancer control. Amongst many reasons, inefficient systemic delivery and bioavailability of promising chemopreventive agents are considered to significantly contribute to such a disconnect. We recently introduced a novel concept in which we utilized nanotechnology for enhancing the outcome of chemoprevention (Cancer Res. 2009; 69:1712-6) and termed it nanochemoprevention. To establish the proof-of-principle of nanotechnology for cancer management, we determined the efficacy of a well-known chemopreventive agent epigallocatechin-3-gallate (EGCG) encapsulated in polylactic acid (PLA)-polyethylene glycol (PEG) nanoparticles in preclinical settings and observed that, compared to non-encapsulated EGCG, nano-EGCG retained its biological efficacy with over 10-fold dose advantage both in cell culture system and in vivo settings in athymic nude mice implanted with human prostate cancer cells. This study laid the foundation of nanochemoprevention by bioactive food components. Since oral consumption is the most desirable and acceptable form of delivery of bioactive food components, it will be important to develop nanoparticles containing bioactive food components that are suitable for oral consumption for which experiments are underway in this laboratory.