Zedoary turmeric oil and its main active ingredient β-elemene are novel plant-derived anticancer agents with long-term clinical application history and low toxicity, which have been approved by the Chinese SFDA to treat different tumors including cancers of the brain, ovary, prostate, breast, lungs, liver, colon, and other tissues. Unfortunately, their hydrophobic properties, poor stabilities and low bioavailabilities seriously hamper their applications in clinic. Therefore, more attention should be paid to develop novel drug delivery systems for zedoary turmeric oil and β-elemene to enhance their overall quality. Recently, increased research has been carried out on a nanoparticle drug delivery system of zedoary turmeric oil and β-elemene to solve their poor aqueous solubilities and low bioavailabilities in vivo with much remarkable achievements springing up in the last decade. This review presents the novel nanoparticle formulations of zedoary turmeric oil and β-elemene and introduces the possible future prospects of their further study. © 2011 World Scientific Publishing Company & Institute for Advanced Research in Asian Science and Medicine.