Optimisation and In Vivo Evaluation of Pectin Based Drug Delivery System Containing Curcumin for Colon

Abstract

The higher incidences of side effects of existing drugs have shifted researchers and clinicians to explore the dietary phytoconstituents for its therapeutic potentials. The present study is based on compression coated curcumin tablet for the colon. Curcumin has anti-inflammatory and antioxidant properties. Curcumin presents a bioavailability problem due to poor solubility. An inclusion complex was formed with hydroxypropyl-β-cyclodextrin to enhance the solubility. In this study, the core tablet of curcumin inclusion complex was compressed between the layers of polymer blend of pectin and Eudragit S100. The 32 full factorial design was utilised for optimization of the formulation. The polymer ratio (X1) and coat thickness (X2) presented significant effects on the selected responses, i.e., percent drug release after 4 hours (Y240) and difference in percent drug release between 4th and 6th hour (Ydiff) in presence of pectinase enzyme. The results revealed that higher coat weight (600 mg) and higher level of pectin ratio (70% w/w) protected the curcumin tablet till ascending colon. The in vivo studies by roentgenography method using human volunteers supported these observations. Hence, it can be concluded that the combination of pectin and Eudrgit S100 makes the system biodegradable and pH dependent for targeting the drug to the colon.