作者：Shan Zhang, Jianbin Xu, Heng Chen*, Zhangfa Song, Yanla Wu, Xingyi Dai and Jie Kong*
关键字：Acid-cleavable， Unimolecular Micelles，Star Copolymers， Triggered Release
论文来源：期刊
具体来源：Macromolecular Bioscience, 2016, in press
发表时间：2017年

Shan Zhang, JianbinXu, Heng Chen*, Zhangfa Song, Yanla Wu, Xingyi Dai and Jie Kong*,

Acid-cleavable Unimolecular Micelles of Amphiphilic Star Copolymers for Potential Triggered Release of Anticancer Drugs, Macromolecular Bioscience, 2016, 2017, 17(3), 10.1002/mabi.201600258

链接：http://onlinelibrary.wiley.com/wol1/doi/10.1002/mabi.201600258/abstract

In this contribution, amphiphilic star copolymers (H40-star-PCL-a-PEG) with an H40 hyperbranched polyester core and poly(ε-caprolactone)-a-poly(ethylene glycol) copolymer arms linked with acetal groups were synthesized using ring-opening polymerization and a copper (I)-catalyzed alkyne-azide cycloaddition (CuAAC) click reaction. The acid-cleavable acetal groups between the hydrophilic and hydrophobic segments of the arms endowed the amphiphilic star copolymers with pH responsiveness. In aqueous solution, unimolecular micelles could be formed with good stability and a unique acid degradability, as is desirable for anticancer drug carriers. For the model drug of doxorubicin, the in vitro release behavior, intracellular release and inhibition of proliferation of HeLa cells showed that the acid-cleavable unimolecular micelles with anticancer activity could be dissociated in an acidic environment and efficiently internalized by HeLa cells. Due to the acid-cleavable and biodegradable nature, unimolecular micelles from amphiphilic star copolymers are promising for applications in intracellular drug delivery for cancer chemotherapy.