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通过 RAFT 聚合合成用于药物输送应用的功能性核、星形聚合物。

Synthesis of functional core, star polymers via RAFT polymerization for drug delivery applications.

机构信息

Australian Centre for Nanomedicine, School of Chemical Engineering, The University of New South Wales, Sydney NSW 2052, Australia.

出版信息

Macromol Rapid Commun. 2012 May 14;33(9):760-6. doi: 10.1002/marc.201200029. Epub 2012 Apr 12.

Abstract

Poly(oligoethylene glycol) methyl ether acrylate was polymerized via reversible addition fragmentation transfer polymerization (RAFT), and then chain extended in the presence of both a cross-linker and vinyl benzaldehyde (VBA), yielding monodisperse star polymers. The presence of aldehyde groups in the core was exploited to attach doxorubicin. The drug loading was controlled by the amount of VBA incorporated (until 28 wt% in drug). The doxorubicin release was studied at pH = 5.5 and 7.4; conditions representative of endosomal and extra cellular environments. In vitro studies revealed that the doxorubicin-conjugated star polymers had a level of cytotoxicity comparable to that found for free doxorubicin. Confocal microscopy and flow cytometry studies confirmed efficient cell uptake of the star polymers.

摘要

聚(聚氧乙烯乙二醇)甲基醚丙烯酸酯通过可逆加成-断裂链转移聚合(RAFT)聚合,然后在交联剂和苯甲醛乙烯基(VBA)的存在下进行链延伸,得到单分散的星形聚合物。核心中醛基的存在被利用来连接阿霉素。药物负载量通过 VBA 的加入量来控制(药物含量高达 28wt%)。在 pH=5.5 和 7.4 下研究了阿霉素的释放;这两种条件分别代表了内涵体和细胞外环境。体外研究表明,与游离阿霉素相比,阿霉素偶联的星形聚合物具有相当的细胞毒性。共聚焦显微镜和流式细胞术研究证实了星形聚合物的有效细胞摄取。

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