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Synthesis of poly(ethylene glycol)-SS-poly(ε-caprolactone)-SS-poly(ethylene glycol)triblock copolymers via end-group conjugation and self-assembly for reductively responsive drug delivery

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Frontiers of Materials Science 2019年第4期13卷 410-419页

作者： Junbo LI Junting JIANG Biyu ZHOU Chaohuang NIU Wendi WANG Wenlan WU School of Chemical Engineering and Pharmaceutics Henan University of Science and TechnologyLuoyang 471023China School of Medicine Henan University of Science and TechnologyLuoyang 471023China

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 ***-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 ***,end-groups conjugation is a simple and straightforward strategy to introduce intelligent responsiveness in biocompatible block copolymers and improve their therapeutic efficacy.

关键词： poly-ε-caprolactone poly(ethylene glycol) block copolymer reductive responsiveness drug release

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Preparation of Composite Particles Made of Biodegradable polymer and a Few Additives with Phase Separation Followed by Drying-in-Liquid

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Journal of Encapsulation and Adsorption Sciences 2015年第1期5卷 11-20页

作者： Mitsuru Kutsuwada Yoshinari Taguchi Masato Tanaka Graduate School of Science and Technology Niigata University Niigata Japan

It was tried to prepare the biodegradable composite particles by the phase separation method followed by the drying-in-liquid method. The composite particles were made of poly-ε-caprolac-tone, quaternary ammonium, carbon black and wax. In the experiment, acetone and water were selected as a good solvent and a poor solvent for poly-ε-caprolactone, quaternary ammonium and wax, respectively. The composite particles were prepared by changing the surfactant species and their concentration, the feeding velocity of water and the weight ratio of poly-ε-caprolactone with larger molecular weight to one with smaller molecular weight. The composite particles with the inner structure in which carbon black, quaternary ammonium and wax were coated well with poly-ε-caprolactone could be prepared by the preparation method presented in this study. The structure and the mean diameter of composite particles were strongly affected by the feeding velocity of water. The higher the feeding velocity of water, the larger the mean diameter of composite particles. The mean diameter was drastically decreased with the surfactant concentration and increased with the added amount of poly-ε-caprolactant with larger molecular weight.

关键词： Biodegradable Composite Particles Phase Separation Drying-in-Liquid poly-ε-caprolactone Microencapsulation

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