Synthesis and evaluation of the 5-fluorouracil-pectin conjugate targeted at the colon

This paper describes the first covalent synthesis of a 5-fluorouracil-pectin (FU-PT) conjugate. This conjugate with the potential for colon-targeted delivery has been evaluated. A sensitive high-performance liquid chromatography (HPLC) method was established for the determination of concentration of 5-FU-1-acetic acid in the gastrointestinal contents and plasma of rats. This method was also used to evaluate the colon-targeting properties of 5-FU-PT. 5-FU-PT was given to rats by oral administration at a dosage of 22.5 mg kg(-1). The different parts of gastrointestinal tract and plasma were taken after 1, 3, 5, 7, 9, 12, 24, 36, and 48 h of oral administration of 5-FU-PT to rats, and the concentration of 5-FU-1-acetic acid in gastrointestinal contents and plasma was measured by HPLC. 5-FU-1-acetic acid released from 5-FU-PT was mainly distributed in the cecum and colon. Therefore, the present results suggest that the 5-FU-PT conjugate has a good colon-targeting property.