pH-Sensitive Drug-Conjugates on Water-Soluble Polymer Frameworks

Title
pH-Sensitive Drug-Conjugates on Water-Soluble Polymer Frameworks
Authors
A. Siddique조영준김유진방승훈김성우이재열강호정김세훈배유한김정안
Keywords
acid-dependent drug-release; living anionic block copolymerization; PEO?drug conjugates; poly(ethylene oxide)- based block copolymers
Issue Date
2015-01
Publisher
Macromolecular chemistry and physics
Citation
VOL 216, 265-276
Abstract
A potent synthetic methodology is introduced to generate a useful intermediate for the preparation of ‘smart’ polymeric pro-drugs. Herein, living anionic block polymerization of ethylene oxide (EO) and N -phenylmaleimide ( N -PMI), as well as the Gabriel process, are introduced. Hydrazinolysis of the resulting poly(ethylene oxide)- block -poly( N -PMI) (PEO- b -P N -PMI) using hydrazine under acidic conditions leads to the production of PEO-based frameworks with hydrazide (HZ) groups. The HZ groups are found to effect the formation of an acidsensitive bond in reactions with medicines or drugs under neutral conditions (pH 7.2). The PEO-HZ intermediate, which shows a strong triplet splitting patterned chemical shift in the range δ = 6.5–8.5 ppm, represents the most powerful material employed for mass production of smart polymeric pro-drugs while controlling the drug-loading yield. Watersoluble “smart” polymeric pro-drugs, such as poly(ethylene oxide)-doxorubicin (PEO-HZ-Dox), poly(ethylene oxide)- methotrexate (PEO-HZ-MTX), and poly(ethylene oxide)-folate (PEO-HZ-FA) conjugates, show excellent acid-sensitive release profi les in water or alcohol at pH 4.5.
URI
http://pubs.kist.re.kr/handle/201004/50615
ISSN
10221352
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KIST Publication > Article
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