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Naproxen-PC: a GI safe and highly effective anti-inflammatory.

L M Lichtenberger¹, J J Romero, E J Dial

¹Department of Integrative Biology & Pharmacology, The University of Texas Health Science Center at Houston, Houston, TX, USA. Lenard.M.Lichtenberger@uth.tmc.edu

Inflammopharmacology

|January 14, 2009

Summary

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Area of Science:

Pharmacology
Gastroenterology
Inflammation Research

Background:

Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used but associated with gastrointestinal (GI) risks.
Naproxen is noted for a favorable cardiovascular safety profile among NSAIDs.
Phosphatidylcholine (PC)-associated NSAIDs are being developed for improved GI safety and efficacy.

Purpose of the Study:

To evaluate the GI safety and anti-inflammatory efficacy of a Naproxen-PC formulation.
To compare Naproxen-PC with conventional naproxen in established rodent models of GI injury and inflammation.

Main Methods:

An acute NSAID-induced intestinal bleeding model in rats.
A chronic inflammation model in rats with pre-existing hindpaw inflammation.
Assessment of GI protection, hindpaw edema, and prostaglandin E2 (PGE2) levels.

Main Results:

Naproxen-PC demonstrated superior GI protection compared to naproxen in both acute and chronic rodent models.
The Naproxen-PC formulation maintained significant anti-inflammatory efficacy, reducing hindpaw edema.
Reduced PGE2 generation was observed in joint synovial fluid with Naproxen-PC treatment.

Conclusions:

Naproxen-PC significantly reduces GI injury and bleeding in rodent models.
The formulation preserves the anti-inflammatory and COX-inhibitory activity of naproxen.
Naproxen-PC represents a promising NSAID with enhanced GI safety.