pH-Sensitive Drug-Conjugates on Water-Soluble Polymer Frameworks
- pH-Sensitive Drug-Conjugates on Water-Soluble Polymer Frameworks
- A. Siddique; 조영준; 김유진; 방승훈; 김성우; 이재열; 강호정; 김세훈; 배유한; 김정안
- acid-dependent drug-release; living anionic block
copolymerization; PEO?drug conjugates; poly(ethylene oxide)-
based block copolymers
- Issue Date
- Macromolecular chemistry and physics
- VOL 216, 265-276
- 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.
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