title: Synthesis and functions of well-defined polymer-drug conjugates as efficient nanocarriers for intravesical chemotherapy of bladder cancer(a).
abstract: Novel poly(ethylene glycol) and poly(N-(2-hydroxypropyl)methacrylamide) block copolymer (PEG-b-PHPMA) with well-defined composition was synthesized by RAFT polymerization. Folate and doxorubicin (DOX) were quantitatively introduced into the copolymer. The influences of folate content and pH value on folate receptor (FR) mediated cell endocytosis and pH-responsive DOX release were studied. It has been demonstrated that minimum folate content is needed for the enrichment of hydrophobic folate on the hydrophilic part of polymer conjugates. The cytotoxicity of targetable polymer drug conjugates was much higher than that of non-targetable ones and free DOX. It could be concluded that the folate plays a significant role in targeting and internalization of the conjugates against bladder cancer cells.
authors.affiliation: State Key Laboratory of Organic-inorganic Composites, Beijing Laboratory of Biomedical Materials, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing, 100029,, China.
authors.forename: Qingsong
authors.initials: Q
authors.lastname: Yu
authors.forename: Jiajing
authors.initials: J
authors.lastname: Zhang
authors.forename: Guan
authors.initials: G
authors.lastname: Zhang
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Gan
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D005492:Folic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D011092:Polyethylene Glycols / Q000737:chemistry / Q000627:therapeutic use; D011108:Polymers / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D011109:Polymethacrylic Acids / Q000737:chemistry; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy* / Q000473:pathology
chemical_list: D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D011109:Polymethacrylic Acids; D011092:Polyethylene Glycols; C011533:Duxon; D004317:Doxorubicin; D005492:Folic Acid
keywords: cancer; chemotherapy; drug conjugates