title: DACHPt-Loaded Unimolecular Micelles Based on Hydrophilic Dendritic Block Copolymers for Enhanced Therapy of Lung Cancer.
abstract: Combining sufficient stability during circulation and desirable drug release is still a great challenge for the clinical applications of nanocarriers. To satisfy this demand, we developed a novel unimolecular micelle (UM) to deliver the antitumor agent 1,2-diaminocyclohexane-platinum(II) (DACHPt) for enhanced therapy of lung cancer. This DACHPt-loaded UM (UM/DACHPt) was formed through chelate complexation between DACHPt and a hydrophilic and biodegradable dendritic block copolymer poly(amidoamine)-polyglutamic acid-b-polyethylene glycol (PAM-PGlu-b-PEG), which was composed of generation 3 PAMAM (PAMAM-G3), polyglutamic acid, and long-circulating polymer PEG. This UM/DACHPt displayed robust stability and would effectively inhibit the undesired release under physiological condition, thus exhibiting much longer in vivo half-life than diblock copolymer micelles. With significant in vitro cell cytotoxicity to A549 lung cancer cells, this UM/DACHPt demonstrated efficient antitumor efficacy on an A549 xenograft tumor model with negligible tissue cytotocxity. Therefore, this UM/DACHPt provides a promising new strategy for lung cancer therapy.
authors.affiliation: The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University , Shenzhen 518055, People's Republic of China.|School of Life Sciences, Tsinghua University , Beijing 100084, People's Republic of China.
authors.forename: Gan
authors.initials: G
authors.lastname: Liu
authors.affiliation: Kingfa Science & Technology Company, Ltd. , Guangzhou 510663, People's Republic of China.
authors.forename: Hongjun
authors.initials: H
authors.lastname: Gao
authors.affiliation: The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University , Shenzhen 518055, People's Republic of China.|School of Life Sciences, Tsinghua University , Beijing 100084, People's Republic of China.
authors.forename: Yixiong
authors.initials: Y
authors.lastname: Zuo
authors.affiliation: The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University , Shenzhen 518055, People's Republic of China.|School of Life Sciences, Tsinghua University , Beijing 100084, People's Republic of China.
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Zeng
authors.affiliation: The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University , Shenzhen 518055, People's Republic of China.|School of Life Sciences, Tsinghua University , Beijing 100084, People's Republic of China.
authors.forename: Wei
authors.initials: W
authors.lastname: Tao
authors.affiliation: The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University , Shenzhen 518055, People's Republic of China.|School of Life Sciences, Tsinghua University , Beijing 100084, People's Republic of China.
authors.forename: Hsiang-I
authors.initials: HI
authors.lastname: Tsai
authors.affiliation: The Shenzhen Key Lab of Gene and Antibody Therapy and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University , Shenzhen 518055, People's Republic of China.|School of Life Sciences, Tsinghua University , Beijing 100084, People's Republic of China.
authors.forename: Lin
authors.identifier: 0000-0001-6503-5149
authors.initials: L
authors.lastname: Mei
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents; D004337:Drug Carriers; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008175:Lung Neoplasms; D008823:Micelles; D011092:Polyethylene Glycols; D011108:Polymers
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D011092:Polyethylene Glycols
keywords: DACHPt; dendritic block copolymers; lung cancer; polyglutamic acid; unimolecular micelles