Development of the PC-NSAID technology: From contact angle to Vazalore®

We describe strategies in drug development to reduce the gastrointestinal (GI) toxicity of nonsteroidal anti-inflammatory drugs (NSAIDs). We then provide an overview of the experiments that led to the development of PC-NSAIDs, a novel family of NSAIDs associated with phosphatidylcholine (PC) that have reduced GI toxicity and full therapeutic activity. Furthermore, we describe the evidence showing: that the stomach possesses hydrophobic properties that are attributable to phospholipids lining the mucus gel layer; and that NSAIDs chemically associate with intrinsic PC, thereby attenuating the tissue's hydrophobic properties. Further, pre-associating NSAIDs with PC reduces the GI toxicity of these drugs, both in rodent ulcer models and in human subjects, without affecting the drugs' therapeutic activity. Finally, we discuss the commercialization and launch of Aspirin-PC, an over-the-counter (OTC) drug with the brand name Vazalore (R).

Automated summary

This article describes strategies in drug development to reduce the gastrointestinal toxicity of NSAIDs. The development of PC-NSAIDs, a new family of NSAIDs associated with phosphatidylcholine that has reduced GI toxicity and full therapeutic activity, is discussed. It is shown that the stomach's hydrophobic properties, attributed to phospholipids, can be attenuated by chemically associating NSAIDs with intrinsic PC. Furthermore, pre-associating NSAIDs with PC reduces GI toxicity without affecting therapeutic activity. The commercialization and launch of Aspirin-PC, an over-the-counter drug with the brand name Vazalore (R), is also discussed.