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Synthesis and Functions of Well‐defined Polymer‐drug Conjugates as Efficient Nanocarriers for Intravesical Chemotherapy of Bladder Cancer a
Author(s) -
Yu Qingsong,
Zhang Jiajing,
Zhang Guan,
Gan Zhihua
Publication year - 2015
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.201400416
Subject(s) - methacrylamide , nanocarriers , chemistry , doxorubicin , conjugate , endocytosis , internalization , copolymer , cytotoxicity , peg ratio , ethylene glycol , raft , polymer , micelle , polymerization , reversible addition−fragmentation chain transfer polymerization , combinatorial chemistry , polymer chemistry , drug delivery , biochemistry , chemotherapy , organic chemistry , cell , radical polymerization , in vitro , aqueous solution , medicine , surgery , mathematical analysis , acrylamide , mathematics , finance , economics
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.