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Original Article

J App Pharm Sci. 2018; 8(11): 95-102


GASTRIC FLOATING IN-SITU GEL AS A STRATEGY FOR IMPROVING ANTI-INFLAMMATORY ACTIVITY OF MELOXICAM

MOHAMMED JAFAR, MOHAMMED SALAHUDDIN, SRINIVASA RAO BOLLA.

Abstract
The present study was aimed to develop gastric floating in-situ gels of meloxicam (MLX) mainly to enhance anti-inflammatory activity and alleviate gastric ulceration potential of meloxicam. Ternary inclusion complex of meloxicam containing hydroxyl propyl beta cyclodextrin (HPβCD) and diethylamine (DEA) in 1:1:1 molar ratio was used as chief component in the development of gastric floating in-situ gel formulations of meloxicam. Box-Behnken design was utilized to design and optimize gastric floating in-situ gels of meloxicam. Independent variables (concentrations of sodium alginate, calcium carbonate, and ternary inclusion complex of meloxicam respectively) were optimized in order to achieve the desired responses. The response surface plots and the possible interactions between the independent variables were analyzed using the Design Expert Software 11.0.3.0 (Stat-Ease, Inc, USA). The results showed that the optimized gastric floating in-situ gels with short floating lag time (41 seconds), low viscosity (190 cps), and high in-vitro drug release at 6th hour (77%) was obtained using an optimized combination of calcium carbonate (0.75%w/v), sodium alginate (1.25%w/v) and MLX-HPβCD-DEA ternary complex (equivalent to 11.25mg of meloxicam), respectively. Moreover, the optimized gastric floating in-situ gel formulation of meloxicam ternary complex exhibited significantly ameliorated anti-inflammatory activity (84.38 % (p

Key words: Meloxicam, Inclusion complex, NSAID, In-situ gel, In-Vivo activity


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