In Vitro and in Vivo Characterization of Sodium Alginate Based in Situ Gelling System of Meloxicam for Stomach Specific Drug Delivery

Abstract

Meloxicam is a non-steroidal anti-inflammatory agent, used in the treatment of rheumatoid arthritis, osteoarthritis, joint diseases and dental pain and in the management of acute post-operative pain. It is selected as model drug candidate because of its wide spectrum of anti-inflammatory activity together with less gastric and local tissue irritation. The present study deals with the development and evaluation of a novel, stomach specific floating in situ gelling system (IGS) of MLX as a means of sustaining the drug release and improving the compliance of dysphagic and geriatric patients who have difficulty in handling and swallowing solid oral dosage forms. The prepared gels were characterized for solution viscosity, floating lag time, physical appearance, water uptake study, in vitro drug release studies. It was observed that both the concentration of sodium alginate and the concentration of calcium carbonate have significant influence on the prepared in situ gelling system characteristics of viscosity, drug content, 50 % and 80 % drug release and similarity factor. In vitro drug release study indicated that the release of the drug from the gel matrix followed non-Fickian diffusion. Pharmacodynamic studies carried out in albino rats revealed significantly increased analgesic/anti-inflammatory response from IGS compared to conventional suspension. Rat pylorus ligation method was employed for in vivo study of the optimized formulation and the results show the formation of gel in gastric juice of the stomach. Studies of the short term stability indicated little or no significant changes. This investigation demonstrates the feasibility of preparing a liquid; stomach specific IGS of MLX for better patient compliance.