Acute and chronic inflammation associated with pain may result in diseases and disorders such as hay fever, atherosclerosis, discrepancy in blood pressure, mental despair, and personality disorganization, if it is not given treatment at the beginning itself. Most anti-inflammatory drugs employed for pain relief intention for long term display extensive adverse reports such as creating renal side effects, gastrointestinal side effects, gastrointestinal bleeding, perforation etc. and few further side effects such as hypersensitivity reactions and distinct salicylate intoxication. Targeting drugs to the inflamed region, in the treatment of rheumatoid arthritis, osteo-arthritis, inflammatory bowel disease and other chronic musculoskeletal conditions would reduce the amount of drug required to control the disease, with possible additional reduction or even elimination of adverse side effects. Novel drug carrier systems are playing an important role in targeting anti-inflammatory drugs to inflamed region. Carriers like liposomes, microspheres, nanoparticles and dendrimer, etc. have shown potential to supplement sustained drug delivery, extended duration of action with improved patient compliance. This review focuses on the current state of the art in the field of nanocarrier mediated controlled and site specific delivery of anti-inflammatory drugs.