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首页> 外文期刊>ACS Macro Letters >Micellar Paclitaxel-Initiated RAFT Polymer Conjugates with Acid-Sensitive Behavior
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Micellar Paclitaxel-Initiated RAFT Polymer Conjugates with Acid-Sensitive Behavior

机译：胶束紫杉醇引发的筏聚合物缀合物与酸敏感行为

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摘要

Acid-sensitive paclitaxel (PTX)–polymer conjugates were designed by applying a grafting-from-drug RAFT approach. PTX was linked through either a cyclic or a linear, acid-sensitive acetal moiety. Relative to direct esterification of PTX, which occurred regioselectively at the C2′ OH-group, direct acetalization was observed at either the C2′ or the C7 OH-group of PTX. This yielded two regioisomers of acetal-based PTX-functionalized RAFT chain transfer agents (CTAs). Subsequent polymerization with N,N-dimethylacrylamide (DMA) resulted in amphiphilic highly defined, acetal-based PTX–polymer conjugates with nearly identical features in terms of polymer definition and micellar self-assembly behavior, but with distinct PTX release kinetics and absence of burst release. This was further reflected by their in vitro biological performance, giving insights into the difference of the release mechanism between ester- and acetal-based PTX–polymer conjugates.]]>
机译：<！[cdata [ src ='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/amlccd/2017/amlccd.2017.7.issue-3/acsmacrolett.6b00977/20170315/通过施加接枝从药物筏方法设计图像/培养基/ MZ-2016-009779_0007.gif“>酸敏感紫杉醇（PTX） - 共聚物缀合物。 PTX通过环状或线性，酸性敏感缩醛部分连接。相对于直接酯化的PTX，其在C 2 'OH-基团上发生区域，在C 2 '或C 7处观察到直接缩醛化 oh-group的ptx。这产生了两种基于缩醛的PTX官能化的筏链转移剂（CTA）的重组分子。随后的聚合与 N， N-I> - 二甲基丙烯酰胺（DMA）导致两亲高定义的缩醛基PTX-聚合物缀合物，具有几乎相同的特征，在聚合物定义和胶束自我方面具有几乎相同的特征 - 组装行为，但具有明显的PTX释放动力学和缺乏爆发释放。这进一步反映了它们的体外的生物学性能，对酯和乙酰基的PTX-聚合物缀合物之间的释放机制的差异进行了洞察。]>

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  • 来源
    《ACS Macro Letters》 |2017年第3期|共5页
  • 作者

    Benoit Louage; Mies J. van Steenbergen; Lutz Nuhn; Martijn D. P. Risseeuw; Izet Karalic; Johan Winne; Serge Van Calenbergh; Wim E. Hennink; Bruno G. De Geest;

  • 作者单位

    Laboratory of Pharmaceutical Technology Department of Pharmaceutics Ghent University Ottergemsesteenweg 460 9000 Ghent Belgium;

    Department of Pharmaceutics Utrecht Institute for Pharmaceutical Sciences Utrecht University Universiteitsweg 99 3584CG Utrecht The Netherlands;

    Laboratory of Pharmaceutical Technology Department of Pharmaceutics Ghent University Ottergemsesteenweg 460 9000 Ghent Belgium;

    Laboratory for Medicinal Chemistry Department of Pharmaceutics Ghent University Ottergemsesteenweg 460 9000 Ghent Belgium;

    Laboratory for Medicinal Chemistry Department of Pharmaceutics Ghent University Ottergemsesteenweg 460 9000 Ghent Belgium;

    Department of Organic and Macromolecular Chemistry Ghent University Krijgslaan 281 S4 9000 Ghent Belgium;

    Laboratory for Medicinal Chemistry Department of Pharmaceutics Ghent University Ottergemsesteenweg 460 9000 Ghent Belgium;

    Department of Pharmaceutics Utrecht Institute for Pharmaceutical Sciences Utrecht University Universiteitsweg 99 3584CG Utrecht The Netherlands;

    Laboratory of Pharmaceutical Technology Department of Pharmaceutics Ghent University Ottergemsesteenweg 460 9000 Ghent Belgium;

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  • 正文语种 eng
  • 中图分类 有机化学;
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