Gelucire BasedIn SituGelling Emulsions: A Potential Carrier for Sustained Stomach Specific Delivery of Gastric Irritant Drugs

Abstract

Non steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed medications to the geriatric patients for the treatment of arthritis and other painful disorders. The major side effects of NSAIDs are related to their effects on the stomach and bowels. The present study concerns assessment of the potential of liquidin situgelling emulsion formulations (emulgels) as patient compliant stomach specific sustained release carrier for the delivery of highly gastric irritant drug, Piroxicam. Emulgels were prepared, without using any emulgent, by mixing different concentrations of molten Gelucire 39/01 with low viscosity sodium alginate solution prepared in deionized water at 50°C. CaCO3was used as buoyancy imparting as well as crosslinking agent. Emulgels so prepared were homogenous, physically stable, and rapidly formed into buoyant gelled mass when exposed to simulated gastric fluid (SGF, pH 1.2). Drug release studies carried out in SGF revealed significant retardation (P<0.05) of Piroxicam release from emulgels compared to conventionalin situgelling formulations prepared without Gelucire 39/01. Pharmacodynamic studies carried out inalbino ratsrevealed significantly increased analgesic/anti-inflammatory response fromin situemulgels compared to conventionalin situgelling formulations. Further,in vivotoxicity studies carried out inalbino ratsrevealed no signs of gastric ulceration upon prolonged dosing.