Formulation Development Of Colon Targeted Release Pellets In Vitro In Vivo Release Study

Abstract

The major endeavor of this study was to develop a more trustworthy and promising, newlinetime-dependent and pH-sensitive combination based drug loaded pellets for effective newlinecolon targeted drug delivery system. Present study aims to formulate the newlinemultiparticulate system comprising of matrix and reservoir type formulation to release newlinethe drug precisely in the colonic site. Along with this, the optimization of variables newlineand parameters of processes such as extrusion-spheronization and Wurster coating newlineusing design of experiments were also aimed. Apart from this, the work also newlineemphasized to carry out in vivo pharmacokinetic study and in vivo X ray imaging or newlineroentgenographic evaluation in rabbits. newlineMETHOD: newline5-FU pellets (Matrix System) newlineThe matrix pellets were prepared by extrusion-spheronization method which is an newlineindustry-accepted method due to its ease of formulation. The prepared pellets were newlinethe matrix of 5-fluorouracil (5-FU) with pH-sensitive and time-dependent polymers, newlinei.e. Eudragit FS30D and Eudragit NM30D respectively. The changing pH media was newlineused for in-vitro release study of optimization batches for both the polymer newlineconcentrations. The Optical microscopy and Scanning electron microscope (SEM) newlinewas used to evaluate texture and surface morphology. newlineThe t10%, t30%, t50%, and t90% values for optimized formulation were extrapolated from newlinein-vitro release vs. time plot which also indicated that the required lag time of 6-8 h newlinewas achieved. The in-vivo roentgenography or X-ray imaging study was used to newlineconfirm the lag time and transition path of colon targeted matrix pellets.In another formulation, the extrusion and spheronization method, preferably newlineemployed in industry for allowing high dose capacity to formulation, was used to newlineprepare 5-aminosalicylic acid (5-ASA) or mesalamine pellets with reservoir type newlineformulation. The Wurster coating technique was used for aqueous coatings of newlineEudragit NE40D as an inner coat and Eudragit FS30D as outer coat. The changing pH newlinemedia was used for in vitro release testing of optimization batc