In this study,we describe a simple synthesis route to prepare triblock copolymers with disulfide-linkers,poly(ethylene glycol)-SS-poly(ε-caprolactone)-SS-poly(ethylene glycol)(PEG-SS-PCL-SS-PEG)for application in the...In this study,we describe a simple synthesis route to prepare triblock copolymers with disulfide-linkers,poly(ethylene glycol)-SS-poly(ε-caprolactone)-SS-poly(ethylene glycol)(PEG-SS-PCL-SS-PEG)for application in the reductively responsive release of doxorubicin(DOX).To synthesize PEG-SS-PCL-SS-PEG,two end-groups of PCL-diol were first modified with cystamine to introduce disulfide bonds and subsequently conjugated with PEG-NHS via carbodiimide chemistry.PEG-SS-PCL-SSPEG fabricated into polymeric micelles with stable structure and different nanoscale sizes via adjusting the PCL chain length,showing obvious reductive responsiveness and fast drug release of encapsulated DOX in the presence of glutathione(GSH).Moreover,DOX-loaded PEG-SS-PCL-SS-PEG micelles exhibited higher therapeutic efficacy than reduction-insensitive PEG-b-PCL micelles in vitro.Thus,end-groups conjugation is a simple and straightforward strategy to introduce intelligent responsiveness in biocompatible block copolymers and improve their therapeutic efficacy.展开更多
基金This work was supported by the National Natural Science Foundation of China(Project U1704150)the Scientific and Technological Projects of Henan Province(182102410017).
文摘In this study,we describe a simple synthesis route to prepare triblock copolymers with disulfide-linkers,poly(ethylene glycol)-SS-poly(ε-caprolactone)-SS-poly(ethylene glycol)(PEG-SS-PCL-SS-PEG)for application in the reductively responsive release of doxorubicin(DOX).To synthesize PEG-SS-PCL-SS-PEG,two end-groups of PCL-diol were first modified with cystamine to introduce disulfide bonds and subsequently conjugated with PEG-NHS via carbodiimide chemistry.PEG-SS-PCL-SSPEG fabricated into polymeric micelles with stable structure and different nanoscale sizes via adjusting the PCL chain length,showing obvious reductive responsiveness and fast drug release of encapsulated DOX in the presence of glutathione(GSH).Moreover,DOX-loaded PEG-SS-PCL-SS-PEG micelles exhibited higher therapeutic efficacy than reduction-insensitive PEG-b-PCL micelles in vitro.Thus,end-groups conjugation is a simple and straightforward strategy to introduce intelligent responsiveness in biocompatible block copolymers and improve their therapeutic efficacy.
