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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Acrylamides / chemical synthesis*
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Acrylamides / chemistry*
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Acrylamides / therapeutic use
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Antibiotics, Antineoplastic / chemical synthesis*
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Antibiotics, Antineoplastic / chemistry*
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Antibiotics, Antineoplastic / therapeutic use
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Cathepsin G / chemistry
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Delayed-Action Preparations / chemical synthesis
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Delayed-Action Preparations / chemistry
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Delayed-Action Preparations / therapeutic use
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Doxorubicin / chemical synthesis*
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Doxorubicin / chemistry*
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Doxorubicin / therapeutic use
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Drug Carriers / chemical synthesis*
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Drug Carriers / chemistry*
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Drug Carriers / therapeutic use
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Maleimides / chemistry
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Oligopeptides / chemistry
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Papain / chemistry
Substances
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Acrylamides
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Antibiotics, Antineoplastic
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Delayed-Action Preparations
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Drug Carriers
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Maleimides
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Oligopeptides
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N-(2-hydroxypropyl)methacrylamide co-polymer-doxorubicin conjugate
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maleimide
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Doxorubicin
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Cathepsin G
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Papain