Curcumin is a principle compound obtained from turmeric, that is, Curcuma longa which is Indian rhizomatous medicinal plant from the family Zingiberaceae. Curcumin is yellow pigment commonly used as a spice in food processing industry. Curcumin, Demethoxycurcumin, and Bisdemethoxycurcumin are the major active constituents of the turmeric and are collectively known as curcuminoids. In recent studies, it has been demonstrated that curcumin has a variety of biological activities, pharmacological performances, provide protection, and promotion of health. This paper reviews the current research progress on its versatile bioactivity, such as antioxidant, anti-inflammatory, and immune-regulatory activities, cancers, diabetes, liver, and cardiovascular systems. The curcumin belongs to biopharmaceutical classification system Class IV that indicates low solubility and low permeability. The systemic bioavailability of orally administered curcumin is low in humans and only traces of it have been found in the liver. Here, we emphasized its broad therapeutic activity in treating life-threatening diseases by improving solubility as well as permeability with the help of novel drug delivery system.