1334238-76-4Relevant academic research and scientific papers
Polymeric drug delivery conjugates and methods of making and using thereof
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Page/Page column 9; 10, (2016/04/20)
Described herein are biodegradable drug delivery conjugates for effectively delivering bioactive agents to a subject. The drug delivery conjugates comprise a water-soluble high molecular weight linear biodegradable polymer backbone comprising a plurality
Synthesis of biodegradable multiblock copolymers by click coupling of RAFT-generated heterotelechelic polyHPMA conjugates
Yang, Jiyuan,Luo, Kui,Pan, Huaizhong,Kope?ková, Pavla,Kope?ek, Jind?ich
experimental part, p. 294 - 302 (2012/01/06)
A new strategy for the synthesis of biodegradable high molecular weight N-(2-hydroxypropyl)methacrylamide (HPMA)-based polymeric carriers has been designed. An enzyme-sensitive, alkyne-functionalized, chain transfer agent (CTA-GFLG-alkyne; Nα-(4-pentynoyl)-Nδ-(4- cyano-4-(phenylcarbonothioylthio)pentanoyl-glycylphenylalanylleucylglycyl) -lysine) was synthesized and used to mediate the reversible addition- fragmentation chain transfer (RAFT) polymerization and copolymerization of HPMA. Post-polymerization modification with 4,4′-azobis(azidopropyl 4-cyanopentanoate) resulted in the formation of heterotelechelic HPMA copolymers containing terminal alkyne and azide groups. Chain extension via click reaction resulted in high molecular weight multiblock copolymers. Upon exposure to papain, these copolymers degraded into the initial blocks. Similar results were obtained for copolymers of HPMA with N- methacryloylglycylphenylalanylleucylglycyl thiazolidine-2-thione and N-methacryloylglycylphenylalanylleucylglycyl-gemcitabine. The new synthetic method presented permits the synthesis of biocompatible, biodegradable high molecular weight HPMA copolymer-anticancer drug conjugates that possess long-circulation times and augmented accumulation in solid tumor tissue due to the enhanced permeability and retention effect.
