title: RGD decoration of PEGylated polyester nanocapsules of perfluorooctyl bromide for tumor imaging: influence of pre or post-functionalization on capsule morphology.
abstract: 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 (19)F 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 (19)F MRI reveals no significant difference of accumulation between PEGylated and RGD-decorated nanocapsules obtained by the post-functionalization approach (highest RGD density/capsule).
authors: Univ Paris-Sud, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France; CNRS UMR 8612, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France.
authors: Odile
authors: O
authors: Diou
authors: Univ Paris-Sud, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France; CNRS UMR 8612, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France.
authors: Elias
authors: E
authors: Fattal
authors: Univ Paris-Sud, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France; CNRS UMR 8612, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France.
authors: Vianney
authors: V
authors: Delplace
authors: Univ Paris-Sud, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France; CNRS UMR 8612, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France.
authors: Nicolas
authors: N
authors: Mackiewicz
authors: Univ Paris-Sud, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France; CNRS UMR 8612, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France.
authors: Julien
authors: J
authors: Nicolas
authors: Commissariat à l'Energie Atomique (CEA), Institut d'Imagerie Biomédicale (I(2)BM), NeuroSpin, CEA Saclay, Gif-sur-Yvette Cedex, France.
authors: Sébastien
authors: S
authors: Mériaux
authors: Commissariat à l'Energie Atomique (CEA), Institut d'Imagerie Biomédicale (I(2)BM), Molecular Imaging Research Center (MIRCen), Fontenay-aux-Roses, France.
authors: Julien
authors: J
authors: Valette
authors: Guerbet, Research Division, Roissy Charles de Gaulle, France.
authors: Caroline
authors: C
authors: Robic
authors: Univ Paris-Sud, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France; CNRS UMR 8612, Institut Galien Paris-Sud, LabEx LERMIT, Châtenay-Malabry, France. Electronic address: nicolas.tsapis@u-psud.fr.
authors: Nicolas
authors: N
authors: Tsapis
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D003287:Contrast Media / Q000737:chemistry*; D020285:Cryoelectron Microscopy; D005260:Female; D066235:Fluorine-19 Magnetic Resonance Imaging / Q000379:methods*; D005466:Fluorocarbons / Q000737:chemistry*; D006842:Hydrocarbons, Brominated; D008819:Mice, Nude; D046529:Microscopy, Electron, Transmission; D053769:Nanocapsules / Q000737:chemistry*; D009369:Neoplasms / Q000175:diagnosis* / Q000378:metabolism / Q000473:pathology; D009842:Oligopeptides / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D013499:Surface Properties
chemical_list: D003287:Contrast Media; D005466:Fluorocarbons; D006842:Hydrocarbons, Brominated; D053769:Nanocapsules; D009842:Oligopeptides; D011092:Polyethylene Glycols; C047981:arginyl-glycyl-aspartic acid; C003072:perflubron
keywords: (19)F MRI; Active targeting; Morphology; PFOB nanocapsules; Polylactide; RGD