Tocotrienols are the major interest of research for their various biological potentials including anticancer activity. They belong to the Vitamin E group of compounds consisting of four isomers. They are obtained from various natural sources including palm oil, rice bran oil, and annatto. However, consuming these sources through diet cannot achieve the desired therapeutic effect due to the poor absorption and distribution of the tocotrienols through gut. It is being challenging since years to increase the bioavailability of tocotrienols so that they can be efficiently taken in the diet. Being lipophilic, they can be absorbed considerably well in the presence of food. Several human and in vivo animal studies indicated the potential of tocotrienols in various medical conditions such as cancer, neuro protection and inflammation. Rigorous research is needed to make them available for the public consumption with proper formulating techniques.