Targeted delivery of resveratrol for colon

Abstract

Despite huge increase in resveratrol solubility by cyclodextrin, bioavailability of resveratrol was not significantly increased, which raised concerns regarding its clinical application. However, resveratrol has therapeutic efficacy on colon cancer and colitis. Therefore, a colon-specific delivery system of resveratrol might be useful to treat these diseases. This study aimed to develop colon-specific delivery systems of resveratrol as calcium-pectinate (Ca-pectinate) and zinc pectinate (Zn-pectinate) beads. However, modification of the pectinate beads was needed to achieve colon-specific delivery of resveratrol. Hence, the beads were hardened by adding polyethyleneimine (PEI) or glutaraldehyde in the cross-linking solution. Several in-vitro studies including drug release study were carried out. In-vivo pharmacokinetic studies in rats were carried out to evaluate the in-vivo efficacy of the optimized formulations. Results showed that resveratrol-loaded Ca-pectinate beads hardened with glutaraldehyde or PEI and resveratrol-loaded Zn-pectinate beads hardened with glutaraldehyde have the potential to be used as colon-specific delivery system of resveratrol.