Disassemblable micelles based on reduction-degradable amphiphilic graft copolymers for intracellular delivery of doxorubicin
Disassemblable micelles based on reduction-degradable amphiphilic graft copolymers for intracellular delivery of doxorubicin
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基于还原可降解两亲接枝共聚物的可拆卸胶束，用于细胞内递送阿霉素
DOI：
10.1016/j.biomaterials.2010.06.011
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发表时间：
2010-09-01
期刊：
影响因子：
14
通讯作者：
Zhang, Xingdong
中科院分区：
文献类型：
--
作者：
Sun, Yong;Yan, Xiaoli;Zhang, Xingdong
基于还原可降解的两亲性聚酰胺胺-g-聚乙二醇接枝共聚物，在整个主链上含有二硫键，开发了用于细胞内递送阿霉素的可拆卸胶束。胶束呈球形，直径小于50 nm，可将阿霉素装入核心，载药量可达20%。胶束在正常生理条件下是稳定的，在还原条件下由于二硫键的断裂而迅速解体。在正常情况下，胶束在24 h内的药物释放量小于25%，而在还原剂DTT存在下，胶束可在10 h内快速释放全部载药。CLSM观察表明，胶束通过内吞作用内化后，可有效地将载药进入细胞核。用人宫颈癌细胞系（HeLa）和人肝癌细胞系（HepG2）证实了载药可拆卸胶束的细胞毒性。(C) 2010 Elsevier Ltd.版权所有。
Disassemblable micelles for intracellular delivery of doxorubicin were developed based on a reduction-degradable amphiphilic polyamide amine-g-polyethylene glycol graft copolymer containing disulfide linkages throughout the main chain. The micelles are spherical of less than 50 nm in diameter, and can load doxorubicin in the core with drug loading content up to 20%. The micelles are stable in normal physiological condition, and quickly disassemble in reductive condition due to the cleavage of the disulfide linkages. The drug release of the micelles in normal condition is less than 25% within 24 h, whereas in the presence of reductive agent, DTT, the micelles can quickly release the entire loaded drug within 10 h. CLSM observation showed that the micelles can effectively deliver the drug cargo into nuclei after internalized through endocytosis. Cytotoxicity of the drug-loaded disassemblable micelles was demonstrated using human cervical cancer cell line (HeLa) and human liver carcinoma cell line (HepG2). (C) 2010 Elsevier Ltd. All rights reserved.