RGD decoration of PEGylated polyester nanocapsules of perfluorooctyl bromide for tumor imaging: Influence of pre or post-functionalization on capsule morphology

PEGylated polyester nanocapsules of perfluorooctyl bromide (PFOB) were surface-decorated with a RGD (arginine-glycine-aspartic acid) peptide by either pre-functionalization or post-functionalization strategies using carbodiimide-assisted chemistry. Both strategies allowed successful linkage of RGD at the surface of nanocapsules with up to 600-950 peptide units per nanocapsule without modifying the encapsulation efficacy of PFOB used as the F-19 MRI imaging moiety. Cryo-Transmission Electron Microscopy images evidence that slight changes of the polymer used to form the capsule shell strongly influence nanocapsule morphology. While, the use of copolymer blends induces the formation of acorn morphologies, PLA-b-PEG-COOH leads to elongated and tears of wine-like nanoconstructs. In vivo evaluation in mice bearing CT26 tumors by F-19 MRI reveals no significant difference of accumulation between PEGylated and RGD-decorated nanocapsules obtained by the post-functionalization approach (highest RGD density/capsule). (C) 2013 Elsevier B.V. All rights reserved.