Being the deadliest disease, cancer is one of the prime concerns for health professionals all over world and thus remarkable research is going on to develop an effective therapy for cancer since many decades. Nutraceuticals have been demonstrated as treatment alternatives for many diseases and also in cancer. Successful outcomes of research regarding applications of naturally available nutraceuticals for various diseases have attracted people to know about and rely more on nutraceuticals for preventive as well as treatment perspective. Potential anticancer activity of many nutraceuticals has demonstrated their important role in cancer therapy; however, associated challenges such as poor solubility, bioavailability, and pharmacokinetic profile restricts their use for prevention and treatment of cancer. Novel drug delivery systems based nanocarrier such as nanoparticles, liposomes, dendrimers, nanoemulsion, and so on have been explored to overcome these challenges for successful delivery of nutraceutical for cancer prevention and treatment. The chapter describes about nutraceutical compound showing anticancer activity, their delivery challenges, and newer approaches of drug delivery systems for nutraceuticals for effective cancer therapy.