Non-steroidal anti-inflammatory drugs (NSAIDs) have been widely used for the management of inflammation, pain and nociception. Gastric intolerance caused by most of the NSAIDs used today restricts their use. Several approaches have been proposed to modify the parent NSAIDs molecule in order to reduce their gastric toxicity. Oral prodrug approach is one of such approaches. This review focuses on the various prodrug approaches used to improve the GI tolerance of NSAIDs.