Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam

Mohammed Jafar; Mohammed Salahuddin; Srinivasa Rao Bolla

doi:10.7324/JAPS.2018.81114

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 hydrox ypropyl beta cyclodextrin (HPβCD) and diethylamine (DEA) in 1:1:1 molar ratio was used as a 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 a 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 a short floating lag time (41 seconds), low viscosity (190 cps), and high in vitro drug release at sixth 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 11.25 mg 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 < 0.05) at sixth hour and also showed a significant reduction in local gastric ulceration potential compared to pure meloxicam]. Thus, this gastric floating in situ gelling system can be translated for existing and established non-steroidal anti-inflammatory drugs (NSAID) as well as formulations.

Keyword: Meloxicam inclusion complex NSAID in-situ gel in vivo activity.

Citation:

Jafar M, Salahuddin M, Bolla SR. Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam. J App Pharm Sci, 2018; 8(11): 095–102.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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