Premium
Synthesis of Long‐Circulating, Backbone Degradable HPMA Copolymer–Doxorubicin Conjugates and Evaluation of Molecular‐Weight‐Dependent Antitumor Efficacy
Author(s) -
Pan Huaizhong,
Sima Monika,
Yang Jiyuan,
Kopeček Jindřich
Publication year - 2013
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201200353
Subject(s) - methacrylamide , raft , conjugate , chemistry , chain transfer , copolymer , doxorubicin , reversible addition−fragmentation chain transfer polymerization , polymer chemistry , radical polymerization , polymer , organic chemistry , chemotherapy , medicine , mathematical analysis , acrylamide , mathematics , surgery
Backbone degradable, linear, multiblock N ‐(2‐hydroxypropyl)methacrylamide (HPMA) copolymer–doxorubicin (DOX) conjugates are synthesized by reversible addition–fragmentation chain transfer (RAFT) polymerization followed by chain extension via thiol‐ene click reaction. The examination of molecular‐weight‐dependent antitumor activity toward human ovarian A2780/AD carcinoma in nude mice reveals enhanced activity of multiblock, second‐generation, higher molecular weight conjugates when compared with traditional HPMA copolymer–DOX conjugates. The examination of body weight changes during treatment indicates the absence of non‐specific adverse effects.