title: Peptide-Based Stealth Nanoparticles for Targeted and pH-Triggered Delivery.
abstract: Stealth agents are extensively investigated as a means by which to prolong nanostructure residence time in the bloodstream by avoiding uptake by the reticuloendothelial system. Unfortunately, commonly used agents such as poly(ethylene glycol) can adversely impact targeting efficiency and promote immune reaction by the host organism. Therefore, there is an increasing interest in developing biocompatible, non-PEGylated organic nanostructures able to perform targeted delivery to increase the efficacy of liposomal technology. Here, a lipopeptide is presented that can be mixed with lipids commonly used in liposomal formulations in percentages ranging from 20% to 60% w/w. The resulting vesicles are thermally and chemically stable. The peptide coating limits serum-protein adsorption even upon prolonged incubation in pure serum in physiological conditions, outperforming PEGylated liposomes. This architecture can be easily modified to allow straightforward derivatization by standard bio-orthogonal conjugation. Upon derivatization with an anti-transferrin receptor aptamer, these vesicles show highly selective cellular internalization with minimal nonspecific uptake and pH-triggered doxorubicin release.
authors.affiliation: NEST, Scuola Normale Superiore and Istituto Nanoscienze-CNR , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Ranalli
authors.affiliation: NEST, Scuola Normale Superiore and Istituto Nanoscienze-CNR , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: Melissa
authors.initials: M
authors.lastname: Santi
authors.affiliation: Center for Nanotechnology Innovation@NEST, Istituto Italiano di Tecnologia , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Capriotti
authors.affiliation: Center for Nanotechnology Innovation@NEST, Istituto Italiano di Tecnologia , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: Valerio
authors.identifier: 0000-0003-1311-3349
authors.initials: V
authors.lastname: Voliani
authors.affiliation: NEST, Scuola Normale Superiore and Istituto Nanoscienze-CNR , Piazza San Silvestro 12, Pisa 56127, Italy.|Center for Nanotechnology Innovation@NEST, Istituto Italiano di Tecnologia , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: David
authors.initials: D
authors.lastname: Porciani
authors.affiliation: NEST, Scuola Normale Superiore and Istituto Nanoscienze-CNR , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: Fabio
authors.initials: F
authors.lastname: Beltram
authors.affiliation: NEST, Scuola Normale Superiore and Istituto Nanoscienze-CNR , Piazza San Silvestro 12, Pisa 56127, Italy.|Center for Nanotechnology Innovation@NEST, Istituto Italiano di Tecnologia , Piazza San Silvestro 12, Pisa 56127, Italy.
authors.forename: Giovanni
authors.identifier: 0000-0002-0067-2240
authors.initials: G
authors.lastname: Signore
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage* / Q000494:pharmacology; D016503:Drug Delivery Systems; D006801:Humans; D008081:Liposomes / Q000737:chemistry*; D008958:Models, Molecular; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy; D010455:Peptides / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D008081:Liposomes; D010455:Peptides; D011092:Polyethylene Glycols; D004317:Doxorubicin