POLYSACCHARIDE-MICROSPONGE BASED MATRIX TABLET FOR COLON TARGETING OF KETOPROFEN: IN VITRO AND IN VIVO EVIDENCE

The present research was aimed to formulate erosion based matrix tablets of ketoprofen micro-sponges for spatial-colon targeting. For the optimization, the effects of independent variables like solvent volume and concentration of chitosan were studied on the mean particle size, percent entrapment efficiency (% EE) and in vitro drug release. Scanning Electron Microscopy (SEM) image of the micro-sponge formulation revealed that the surface of the micro-sponge was nearly spherical and porous. Optimized micro-sponge formulation was further formulated into erosion based matrix tablet and evaluated for quality control parameters. In vitro release studies revealed that both the micro-sponge formulation and micro-sponge matrix tablet (MST) had restricted the drug release of ketoprofen in gastric pH followed by gradual release up to 12 hr. The release kinetics data, after fitting into various models revealed that both formulations were best fitted to zero order, indicating controlled release property. The pharmacokinetic evaluation of colon targeted MST in rats revealed the presence of drug in plasma after lag time of 4 hr, t_max of 4 ± 0.23, AUC (0-12hr) of 33.10 ± 3.68 with t_1/2 3.85 ± 0.31. The developed MST of ketoprofen has the ability for spatial and temporal delivery, thus could be employed to treat various colonic diseases.