Curcumin is the main component in turmeric. It has been used as a food and as a medicinal agent in the Indo-Asian region from time immemorial. Curcumin has been reported to have anti-cancer, anti-inflammatory, anti-microbial, anti-oxidant, and anti-viral bioactivities. It has been widely researched and clinical studies have been conducted to establish the potency of curcumin as a useful therapeutic and nutraceutical. One of the main drawbacks in assessing its biological activity is the insolubility of curcumin which results in its poor bioavailability. Many attempts have been made to improve the bioavailability of curcumin to increase its potency. Encapsulation is a technique that allows increased solubility of lipophilic substances like curcumin. Encapsulation produces microparticles and nanoparticles, of which improved potency of encapsulants has been observed to a greater extent at the nano level. Several encapsulants have been used for this purpose, and are described herein. Among the many methods used to enhance the bioactivity of curcumin are incorporation in o/w nanoemulsions and liposomes. Formation of cocrystals, and other biological and chemical methods, including modification and conjugation for improving bioactivity, are also reviewed.