中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Fabrication of Hyperbranched Block-Statistical Copolymer-Based Prodrug with Dual Sensitivities for Controlled Release

文献类型:期刊论文

作者Zheng, Luping1,2; Wang, Yunfei1,2; Zhang, Xianshuo1,2; Ma, Liwei1,2; Wang, Baoyan1,2; Ji, Xiangling3; Wei, Hua1,2
刊名BIOCONJUGATE CHEMISTRY
出版日期2018
卷号29期号:1页码:190-202
ISSN号1043-1802
DOI10.1021/acs.bioconjchem.7b00699
英文摘要Dendrimer with hyperbranched structure and multivalent surface is regarded as one of the most promising candidates close to the ideal drug delivery systems, but the clinical translation and scale-up production of dendrimer has been hampered significantly by the synthetic difficulties. Therefore, there is considerable scope for the development of novel hyperbranched polymer that can not only address the drawbacks of dendrimer but maintain its advantages. The reversible addition-fragmentation chain transfer self-condensing vinyl polymerization (RAFT-SCVP) technique has enabled facile preparation of segmented hyperbranched polymer (SHP) by using chain transfer monomer (CTM)-based double-head agent during the past decade. Meanwhile, the design and development of block-statistical copolymers has been proven in our recent studies to be a simple yet effective way to address the extracellular stability vs intracellular high delivery efficacy dilemma. To integrate the advantages of both hyperbranched and block-statistical structures, we herein reported the fabrication of hyperbranched block-statistical copolymer-based prodrug with pH and reduction dual sensitivities using RAFT-SCVP and post-polymerization click coupling. The external homo oligo(ethylene glycol methyl ether methacrylate) (OEGMA) block provides sufficient extracellularly colloidal stability for the nanocarriers by steric hindrance, and the interior OEGMA units incorporated by the statistical copolymerization promote intracellular drug release by facilitating the permeation of GSH and H+ for the cleavage of the reduction-responsive disulfide bond and pH-liable carbonate link as well as weakening the hydrophobic encapsulation of drug molecules. The delivery efficacy of the target hyperbranched block-statistical copolymer-based prodrug was evaluated in terms of in vitro drug release and cytotoxicity studies, which confirms both acidic pH and reduction-triggered drug release for inhibiting proliferation of HeLa cells. Interestingly, the simultaneous application of both acidic pH and GSH triggers promoted significantly the cleavage and release of CPT compared to the exertion of single trigger. This study thus developed a facile approach toward hyperbranched polymer-based prodrugs with high therapeutic efficacy for anticancer drug delivery.
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000423012800023
源URL[http://ir.iccas.ac.cn/handle/121111/45395]  
专题中国科学院化学研究所
通讯作者Wei, Hua
作者单位1.Lanzhou Univ, Key Lab Nonferrous Met Chem & Resources Utilizat, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China
2.Lanzhou Univ, Coll Chem & Chem Engn, Lanzhou 730000, Gansu, Peoples R China
3.Chinese Acad Sci, Changchun Inst Appl Chem, State Key Lab Polymer Phys & Chem, Changchun 130022, Peoples R China
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GB/T 7714
Zheng, Luping,Wang, Yunfei,Zhang, Xianshuo,et al. Fabrication of Hyperbranched Block-Statistical Copolymer-Based Prodrug with Dual Sensitivities for Controlled Release[J]. BIOCONJUGATE CHEMISTRY,2018,29(1):190-202.
APA Zheng, Luping.,Wang, Yunfei.,Zhang, Xianshuo.,Ma, Liwei.,Wang, Baoyan.,...&Wei, Hua.(2018).Fabrication of Hyperbranched Block-Statistical Copolymer-Based Prodrug with Dual Sensitivities for Controlled Release.BIOCONJUGATE CHEMISTRY,29(1),190-202.
MLA Zheng, Luping,et al."Fabrication of Hyperbranched Block-Statistical Copolymer-Based Prodrug with Dual Sensitivities for Controlled Release".BIOCONJUGATE CHEMISTRY 29.1(2018):190-202.

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来源:化学研究所

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