Extensive research over the past half century has shown that curcumin (diferuloylmethane), a polyphenolic compound of turmeric (Curcuma longa L.), can modulate multiple cell signaling pathways. Extensive clinical trials have addressed the pharmacokinetics, safety, and efficacy of this nutraceutical against numerous diseases in human. Curcumin, known for thousand years as a subject of Ayurvedic medicine, has undergone in recent times remarkable transformation into a drug candidate with prospective multipotent therapeutic application. Characterized by high chemical reactivity, resulting from an extended conjugated double bond system prone to nucleophilic attack, curcumin has been shown to interact with a plethora of molecular targets, in numerous experimental observations. In clinical trials, has been used either alone or in combination with other agent. However, its clinical advance has been limited by its short biological half-life, fast metabolism and poor systemic bioavailability after oral administration. To mitigate the above limitations, recently various formulation of curcumin, including nanoparticles, micelles, liposomes, phytosomes delivery system has been examined. The present review has been devoted towards better understanding of the phytonutraceutic properties of curcumin and turmeric based on their disease specific indications and enhancing their prophylactic and therapeutic nutraceutical qualities. The article deals with the biological activity, mode of action, toxicity and forthcoming application of these leads.