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Nanoparticle NSAIDs Get ‘Patent Pending’ Status

Commercial licensing expected by second quarter of 2015

The U.S. Patent and Trademark office has issued a “patent pending” designation for the nonsteroidal anti-inflammatory drug (NSAID) NanoSphere technology platform.

The new technology is the first to encapsulate prescription and over-the-counter (OTC) NSAIDs, such as ibuprofen, aspirin, and naproxen, as a method to treat and prevent inflammatory disorders and global inflammation and pain.

According to the system’s developer (NanoSphere Health Sciences), the use of the NanoSphere delivery technology eliminates or alleviates many of the adverse effects that NSAIDs can have, such as gastric irritation and gastric or gastrointestinal (GI) bleeding. At the same time, it increases the therapeutic activity of NSAIDs for safer and more-effective long-term therapy.

NanoSphere NSAIDs are designed to be administered intraorally, intranasally, and transdermally. The liquid nanogels bypass the GI tract, thereby avoiding GI irritation. When taken orally, the nanogels’ structure of purified essential phospholipids maintains the protective GI-tract mucosa barrier from damage by NSAIDs. The nanogels are then transported into the circulatory system for greater therapeutic activity in treating inflammatory conditions and in relieving pain.

NSAIDs can cause a range of GI problems, from a mildly upset stomach to serious conditions, such as gastric bleeding, gastric ulcers, and kidney damage –– factors that often limit NSAID use. Among patients using these drugs, 30% to 40% have some degree of GI intolerance. NSAIDs physically damage the protective GI mucosal surface and promote bleeding. Further, NSAIDs are fat-soluble drugs with low solubility and dissolution in water. This makes OTC and prescription NSAID pills difficult to absorb and contributes to the likelihood of GI problems.

According to Nanophere Health, its phospholipid nanoparticle encapsulation process provides the following potential benefits:

  • Increased concentrations and bioavailability of NSAIDs
  • Decreased dosage of NSAIDS
  • Reduced risk of GI problems
  • Transport into and targeting of specific body sites
  • Delivery into the central nervous system
  • Enhanced therapeutic value
  • Suitability for daily and long-term use

NanoSphere Health Sciences expects commercial licensing to be available by the second quarter of 2015, after clinical trials have been completed.

Source: PR Newswire; January 13, 2015.

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