IN vitro and in vivo evaluation of novel ocular delivery system of 5-fluorouracil peptide hydrogel

Abstract

A novel biocompatible hydrogel was prepared based on the supramolecular self-assembly of a peptide containing a bioactive RGD (arginine-glycine-aspartic acid) sequence and a hydrophobic N-fluorenyl-9-methoxycarbonyl (FMOC) tail. The in vitro biocompatibility assay demonstrated that such self-assembled peptide hydrogel had a well biocompatibility. When intraoperatively administrating the self-assembled peptide hydrogel containing 5-fluorouracil in the filtering surgery of rabbit eyes, quantitative determination of 5-fluorouracil in the aqueous humor showed detectable amounts of 5-fluorouracil (below 1μg/mL) for 1 weeks, which shows that peptide hydrogel was still present in the subconjunctival space for that period and released 5-fluorouracil in a continuous fashion. Attributed to the sustained release of 5-fluorouracil from the hydrogel, the injection of the self-assembled peptide hydrogel containing 5-fluorouracil at surgery site had potential advantages including preventing the frequent 5-fluorouracil injections and the toxicity of 5-fluorouracil to the surrounding ocular tissues efficiently, indicating a potential application of the self-assembled peptide hydrogel as an implanted drug delivery system for the treatment of scarring formation after filtering surgery.