Turmeric (Zingiberaceae) rhizomes have been used for centuries in the indigenous medicine system to treat various inflammatory conditions and other diseases. Its medicinal properties have been attributed mainly due to Curcumin amongst the curcuminoids and the other phytochemicals present in the rhizomes and possess a range of pharmacological activities, including anti-inflammatory, anticancer, antioxidant, wound healing and antimicrobial effects. The other salient feature of turmeric/curcumin is that despite being consumed daily for centuries in Asian countries, it has not been reported to cause any toxicity.The only therapeutic limitation of curcumin is its bioavailability. Curcumin needs be bioaccessible before reaching systemic circulation since bioaccessibility is directly proportional to the solubility of the drug in gastrointestinal fluid. A fraction of curcumin would get intracellular space after it has been ingested. Through a Michael reaction α,β-unsaturated C=O group can produce covalently bonded intracellular protein conjugates with protein thiols. This, could be a reason for a small amount of free curcumin in circulation. To enhance the bioavailability and thus its therapeutic efficacy, researchers are making several efforts all over the globe to develop novel nano-drug delivery systems. This review is concentrated on describing issues linked to curcumin’s poor bioavailability based on its chemical factors, physiological barriers and pharmacokinetics, focusing on its degradation as well as many unformulated and formulated ways utilized to improve its therapeutic effects such as inhibition of pglycoprotein pump, enhancing tight junction integrity as well as the incorporation of curcumin in nanocrystals, cyclodextrin nanoparticles, nanospheres, nanofibers, nanoemulgels, intelligent films, quantum dots etc.