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

Mohammed Jafar, Mohammed Salahuddin, Srinivasa Rao Bolla

Research output: Contribution to journalArticle

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Abstract

The present study was aimed to develop gastric floating in-situ gels of meloxicam (MLX) mainly to enhance antiinflammatory 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.

Original languageEnglish
Pages (from-to)95-102
Number of pages8
JournalJournal of Applied Pharmaceutical Science
Volume8
Issue number11
DOIs
Publication statusPublished - Nov 1 2018
Externally publishedYes

Fingerprint

meloxicam
Stomach
Anti-Inflammatory Agents
Gels
Calcium Carbonate
Software Design

Keywords

  • In vivo activity
  • In-situ gel
  • Inclusion complex
  • Meloxicam
  • NSAID

ASJC Scopus subject areas

  • Medicine (miscellaneous)
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Pharmacology (medical)

Cite this

Gastric floating in-situ gel as a strategy for improving anti-inflammatory activity of meloxicam. / Jafar, Mohammed; Salahuddin, Mohammed; Bolla, Srinivasa Rao.

In: Journal of Applied Pharmaceutical Science, Vol. 8, No. 11, 01.11.2018, p. 95-102.

Research output: Contribution to journalArticle

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abstract = "The present study was aimed to develop gastric floating in-situ gels of meloxicam (MLX) mainly to enhance antiinflammatory 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.",
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