title: Tumour homing and therapeutic effect of colloidal nanoparticles depend on the number of attached antibodies.
abstract: Active targeting of nanoparticles to tumours can be achieved by conjugation with specific antibodies. Specific active targeting of the HER2 receptor is demonstrated in vitro and in vivo with a subcutaneous MCF-7 breast cancer mouse model with trastuzumab-functionalized gold nanoparticles. The number of attached antibodies per nanoparticle was precisely controlled in a way that each nanoparticle was conjugated with either exactly one or exactly two antibodies. As expected, in vitro we found a moderate increase in targeting efficiency of nanoparticles with two instead of just one antibody attached per nanoparticle. However, the in vivo data demonstrate that best effect is obtained for nanoparticles with only exactly one antibody. There is indication that this is based on a size-related effect. These results highlight the importance of precisely controlling the ligand density on the nanoparticle surface for optimizing active targeting, and that less antibodies can exhibit more effect.
authors.affiliation: Dipartimento di Biotecnologie e Bioscienze, Università di Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.
authors.forename: Miriam
authors.identifier: 0000-0003-3428-5668
authors.initials: M
authors.lastname: Colombo
authors.affiliation: Ospedale L. Sacco, Via G. B. Grassi 74, 20157 Milano, Italy.
authors.forename: Luisa
authors.initials: L
authors.lastname: Fiandra
authors.affiliation: Dipartimento di Biotecnologie e Bioscienze, Università di Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.|Dipartimento di Scienze Biomediche e Cliniche 'Luigi Sacco', Università di Milano, Via G. B. Grassi 74, 20157 Milano, Italy.
authors.forename: Giulia
authors.initials: G
authors.lastname: Alessio
authors.affiliation: Ospedale L. Sacco, Via G. B. Grassi 74, 20157 Milano, Italy.|Dipartimento di Scienze Biomediche e Cliniche 'Luigi Sacco', Università di Milano, Via G. B. Grassi 74, 20157 Milano, Italy.
authors.forename: Serena
authors.identifier: 0000-0001-6904-8895
authors.initials: S
authors.lastname: Mazzucchelli
authors.affiliation: Ospedale L. Sacco, Via G. B. Grassi 74, 20157 Milano, Italy.|Dipartimento di Scienze Biomediche e Cliniche 'Luigi Sacco', Università di Milano, Via G. B. Grassi 74, 20157 Milano, Italy.
authors.forename: Manuela
authors.initials: M
authors.lastname: Nebuloni
authors.affiliation: Ospedale L. Sacco, Via G. B. Grassi 74, 20157 Milano, Italy.
authors.forename: Clara
authors.initials: C
authors.lastname: De Palma
authors.affiliation: Fachbereich Physik, Philipps Universität Marburg, Renthof 7, 35037 Marburg, Germany.
authors.forename: Karsten
authors.initials: K
authors.lastname: Kantner
authors.affiliation: Fachbereich Physik, Philipps Universität Marburg, Renthof 7, 35037 Marburg, Germany.
authors.forename: Beatriz
authors.initials: B
authors.lastname: Pelaz
authors.affiliation: Dipartimento di Biotecnologie e Bioscienze, Università di Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.
authors.forename: Rany
authors.initials: R
authors.lastname: Rotem
authors.affiliation: Dipartimento di Scienze Biomediche e Cliniche 'Luigi Sacco', Università di Milano, Via G. B. Grassi 74, 20157 Milano, Italy.|Surgery Department, Breast Unit, ICS Maugeri S.p.A. SB, Via S. Maugeri, 10-27100 Pavia, Italy.
authors.forename: Fabio
authors.initials: F
authors.lastname: Corsi
authors.affiliation: Fachbereich Physik, Philipps Universität Marburg, Renthof 7, 35037 Marburg, Germany.|CIC Biomagune, Miramon Pasealekua 182, 20009 San Sebastian, Spain.
authors.forename: Wolfgang J
authors.identifier: 0000-0003-1672-6650
authors.initials: WJ
authors.lastname: Parak
authors.affiliation: Dipartimento di Biotecnologie e Bioscienze, Università di Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.
authors.forename: Davide
authors.initials: D
authors.lastname: Prosperi
mesh_terms: D000818:Animals; D000906:Antibodies / Q000008:administration & dosage* / Q000276:immunology; D000911:Antibodies, Monoclonal; D045744:Cell Line, Tumor; D002470:Cell Survival; D003102:Colloids; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D007167:Immunotherapy / Q000379:methods; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage*; D009374:Neoplasms, Experimental / Q000628:therapy*
chemical_list: D000906:Antibodies; D000911:Antibodies, Monoclonal; D003102:Colloids; D004337:Drug Carriers