Self nanoemulsifying granules (SNEGs) of meloxicam: preparation, characterization, molecular modeling and evaluation of in vivo anti-inflammatory activity

Abstract

Meloxicam, a BCS class II drug belonging to the class of NSAIDs is indicated in conditions of rheumatoid arthritis, ankylosing spondylitis and osteoarthritis in which rapid onset of drug action is desired to reduce inflammation and pain. The objective of the study was to thus develop Self Nanoemulsifying Granules (SNEGs) of Meloxicam (MLX) for enhancement of solubility; and subsequently dissolution rate, thus aiming for a faster onset of action. Preliminary studies along with molecular modeling studies were carried out for selection of appropriate lipids, surfactants and cosurfactants for the development of MLX-loaded Self Nanoemulsifying preconcentrate (SNEP). A charge inducer was incorporated into the formulation so as to increase the solubility of MLX in lipids and hence, drug loading. A three-factor D-optimal mixture design was used for optimization of MLX loaded SNEP. The role of charge inducer in increasing the drug loading of MLX in SNEDDS was studied by molecular dynamics simulation using Desmond. Optimized SNEP was adsorbed onto solid carriers to form SNEGs for improved stability and enhanced flow properties. Physical characterization studies of SNEGs, in vitro release studies, and in vivo evaluation of anti-inflammatory activity of the optimized formulation were performed. All the results indicated that MLX SNEGs can be a promising alternative to conventional oral NSAIDs therapy because of enhanced dissolution characteristics and subsequent rapid onset of action.

Keywords:

• Meloxicam
• D-optimal mixture design
• stearylamine
• Self Nanoemulsifying Drug Delivery Systems
• Aeroperl® 300 pharma
• Desmond

Acknowledgements

Authors would like to thank Venus Pharmaceuticals Ltd, Mumbai, India for providing gift samples of Meloxicam and Tata Institute of Fundamental Research (TIFR), Mumbai, India for help during XRD studies, and All India Council of Technical Education (AICTE) for providing fellowship.

Disclosure statement

The authors report no declaration of interest.

Funding

This work was supported by University Grant Commission, India [Letter no. F3-10/13; WRO/policy, MRP/SEM XII plan dated February 20, 2015 (File no. 47-993/14)].