title: Anticancer drug nanomicelles formed by self-assembling amphiphilic dendrimer to combat cancer drug resistance.
abstract: Drug resistance and toxicity constitute challenging hurdles for cancer therapy. The application of nanotechnology for anticancer drug delivery is expected to address these issues and bring new hope for cancer treatment. In this context, we established an original nanomicellar drug delivery system based on an amphiphilic dendrimer (AmDM), which could generate supramolecular micelles to effectively encapsulate the anticancer drug doxorubicin (DOX) with high drug-loading capacity (>40%), thanks to the unique dendritic structure creating large void space for drug accommodation. The resulting AmDM/DOX nanomicelles were able to enhance drug potency and combat doxorubicin resistance in breast cancer models by significantly enhancing cellular uptake while considerably decreasing efflux of the drug. In addition, the AmDM/DOX nanoparticles abolished significantly the toxicity related to the free drug. Collectively, our studies demonstrate that the drug delivery system based on nanomicelles formed with the self-assembling amphiphilic dendrimer constitutes a promising and effective drug carrier in cancer therapy.
authors.affiliation: Chinese Academy of Sciences Key Laboratory for Biological Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Chinese Academy of Sciences, 100190 Beijing, People's Republic of China; Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille, UMR 7325, 13288 Marseille, France; Centre de Recherche en Cancérologie de Marseille, INSERM U1068, F-13009 Marseille, France; Institut Paoli-Calmettes, F-13009 Marseille, France; Aix-Marseille Université, F-13284 Marseille, France; CNRS UMR7258, F-13009 Marseille, France; University of Chinese Academy of Sciences, 100049 Beijing, People's Republic of China;
authors.forename: Tuo
authors.initials: T
authors.lastname: Wei
authors.affiliation: Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille, UMR 7325, 13288 Marseille, France; Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire, UMR 7273, 13390 Marseille, France;
authors.forename: Chao
authors.initials: C
authors.lastname: Chen
authors.affiliation: Chinese Academy of Sciences Key Laboratory for Biological Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Chinese Academy of Sciences, 100190 Beijing, People's Republic of China; Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille, UMR 7325, 13288 Marseille, France; University of Chinese Academy of Sciences, 100049 Beijing, People's Republic of China;
authors.forename: Juan
authors.initials: J
authors.lastname: Liu
authors.affiliation: Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille, UMR 7325, 13288 Marseille, France; College of Chemistry and Molecular Sciences, Wuhan University, 430072 Wuhan, People's Republic of China;
authors.forename: Cheng
authors.initials: C
authors.lastname: Liu
authors.affiliation: Molecular Simulation Engineering Laboratory, Department of Engineering and Architecture, University of Trieste, 34127 Trieste, Italy; and.
authors.forename: Paola
authors.initials: P
authors.lastname: Posocco
authors.affiliation: Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille, UMR 7325, 13288 Marseille, France; Centre de Recherche en Cancérologie de Marseille, INSERM U1068, F-13009 Marseille, France; Institut Paoli-Calmettes, F-13009 Marseille, France; Aix-Marseille Université, F-13284 Marseille, France; CNRS UMR7258, F-13009 Marseille, France;
authors.forename: Xiaoxuan
authors.initials: X
authors.lastname: Liu
authors.affiliation: Laboratory of Nucleic Acid Technology, Institute of Molecular Medicine, Peking University, 100871 Beijing, People's Republic of China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Cheng
authors.affiliation: Chinese Academy of Sciences Key Laboratory for Biological Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Chinese Academy of Sciences, 100190 Beijing, People's Republic of China; University of Chinese Academy of Sciences, 100049 Beijing, People's Republic of China;
authors.forename: Shuaidong
authors.initials: S
authors.lastname: Huo
authors.affiliation: Laboratory of Nucleic Acid Technology, Institute of Molecular Medicine, Peking University, 100871 Beijing, People's Republic of China.
authors.forename: Zicai
authors.initials: Z
authors.lastname: Liang
authors.affiliation: Molecular Simulation Engineering Laboratory, Department of Engineering and Architecture, University of Trieste, 34127 Trieste, Italy; and.
authors.forename: Maurizio
authors.initials: M
authors.lastname: Fermeglia
authors.affiliation: Molecular Simulation Engineering Laboratory, Department of Engineering and Architecture, University of Trieste, 34127 Trieste, Italy; and.
authors.forename: Sabrina
authors.identifier: http://orcid.org/0000-0001-8380-4474
authors.initials: S
authors.lastname: Pricl
authors.affiliation: Chinese Academy of Sciences Key Laboratory for Biological Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Chinese Academy of Sciences, 100190 Beijing, People's Republic of China; ling.peng@univ-amu.fr liangxj@nanoctr.cn.
authors.forename: Xing-Jie
authors.initials: XJ
authors.lastname: Liang
authors.affiliation: Centre de Recherche en Cancérologie de Marseille, INSERM U1068, F-13009 Marseille, France; Institut Paoli-Calmettes, F-13009 Marseille, France; Aix-Marseille Université, F-13284 Marseille, France; CNRS UMR7258, F-13009 Marseille, France;
authors.forename: Palma
authors.initials: P
authors.lastname: Rocchi
authors.affiliation: Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille, UMR 7325, 13288 Marseille, France; ling.peng@univ-amu.fr liangxj@nanoctr.cn.
authors.forename: Ling
authors.initials: L
authors.lastname: Peng
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D050091:Dendrimers / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D019008:Drug Resistance, Neoplasm; D006801:Humans; D061986:MCF-7 Cells; D008823:Micelles; D049329:Nanostructures; D014018:Tissue Distribution
chemical_list: D000903:Antibiotics, Antineoplastic; D050091:Dendrimers; D008823:Micelles; D004317:Doxorubicin
keywords: amphiphilic dendrimers; cancer treatment; drug delivery; nanodrugs; supramolecular nanomicelles