Microbeads: a novel multiparticulate drug delivery technology for increasing the solubility and dissolution of celecoxib

Abstract

The purpose of this study was to develop a novel multipaticulate drug delivery technology suitable for the delivery of pre-solubilized celecoxib to the gastrointestinal tract and more specifically to the colon. The solubility of celecoxib in a range of oils, surfactants and co-solvents was evaluated. Celecoxib was solubilized in mixtures of these vehicles to produce liquid formulations. The in vitro dissolution of these liquid formulations was assessed and the data obtained was used to design microbead formulations containing celecoxib dissolved within an emulsion/micellar solution core. Microbead formulations were optimized to increase drug loading, avoid precipitation and to achieve good in vitro dissolution performance. An optimized formulation with a celecoxib loading of 6% w/w was produced and yielded an in vitro dissolution result of 80% over 6 h. The structure of these microbead formulations was characterized using light microscopy to reveal a correlation between droplet size and dissolution performance.

• Drug delivery
• dissolution
• formulation
• solubility

Declaration of interest

The authors report no declaration of interest. The authors would like to acknowledge the funding of this research by the Irish Research Council for Science, Engineering and Technology (IRCSET) and Sigmoid Pharma (Ref IRCSET, Sigmoid, 2009-01).