IN-VIVO ROENTGENOGRAPHIC EVALUATION OF COLON TARGETED 5-FLUOROURACIL PELLETS

Objective: This study was an attempt to explore the latent of colon specificity approach utilizing pH-sensitive and time-dependent characteristics of polymers for defined colonic release of 5-Fluorouracil (5-FU). Method: The pellets were prepared by extrusion-spheronization method which is an industry-accepted method due to its ease of formulation. The prepared pellets were the matrix of 5-Fluorouracil with pH-sensitive and time-dependent polymers, i.e. Eudragit FS30D and Eudragit NM30D respectively. The changing pH media used for in-vitro release study of optimization batches for both the polymer concentrations. The Optical microscopy and Scanning electron microscope (SEM) was used to evaluate texture and surface morphology. Results: The t_10%, t_30%, t_50%, and t_90% values for optimized formulation were found as 2.7 h, 6.2 h, 8.7 h and 18.2 h respectively. These values were extrapolated from in-vitro release vs. time plot which also indicated that the required lag time of 6-8 h was achieved. The in-vivo roentgenography or X-ray imaging study was used to confirm the lag time and transition path of colon targeted matrix pellets. Conclusion: The present study provides assurance for colon targeting of 5-FU pellets with industrially feasible processes. The combination of pH-sensitive and time-dependent polymers in development of pellets contributed to promising and precise drug release at colonic site. The in-vivo roentgenography study also further strengthen proposal of 6-8 h of lag time which was determined based on the in-vitro drug release study.