title: Backbone degradable multiblock N-(2-hydroxypropyl)methacrylamide copolymer conjugates via reversible addition-fragmentation chain transfer polymerization and thiol-ene coupling reaction.
abstract: Telechelic water-soluble HPMA copolymers and HPMA copolymer-doxorubicin (DOX) conjugates have been synthesized by RAFT polymerization mediated by a new bifunctional chain transfer agent (CTA) that contains an enzymatically degradable oligopeptide sequence. Postpolymerization aminolysis followed by chain extension with a bis-maleimide resulted in linear high molecular weight multiblock HPMA copolymer conjugates. These polymers are enzymatically degradable; in addition to releasing the drug (DOX), the degradation of the polymer backbone resulted in products with molecular weights similar to the starting material and below the renal threshold. The new multiblock HPMA copolymers hold potential as new carriers of anticancer drugs.
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, Utah 84112, United States.
authors.forename: Huaizhong
authors.initials: H
authors.lastname: Pan
authors.forename: Jiyuan
authors.initials: J
authors.lastname: Yang
authors.forename: Pavla
authors.initials: P
authors.lastname: Kopecková
authors.forename: Jindrich
authors.initials: J
authors.lastname: Kopecek
mesh_terms: D000178:Acrylamides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000627:therapeutic use; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000737:chemistry* / Q000627:therapeutic use; D056649:Cathepsin G / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D004317:Doxorubicin / Q000138:chemical synthesis* / Q000737:chemistry* / Q000627:therapeutic use; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry* / Q000627:therapeutic use; D008301:Maleimides / Q000737:chemistry; D009842:Oligopeptides / Q000737:chemistry; D010206:Papain / Q000737:chemistry
chemical_list: D000178:Acrylamides; D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008301:Maleimides; D009842:Oligopeptides; C482378:N-(2-hydroxypropyl)methacrylamide co-polymer-doxorubicin conjugate; C043592:maleimide; D004317:Doxorubicin; D056649:Cathepsin G; D010206:Papain