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Steric Protected and Illumination-Activated Tumor Targeting Accessory for Endowing Drug-Delivery Systems with Tumor Selectivity

机译:立体选择性保护和照明激活的肿瘤靶向附件,赋予肿瘤选择性药物输送系统

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摘要

Here, an ABA-typed polymer, octadecyl-polyethylene glycol (biotin)-(o-nitrobenzyl)-octadecyl ester (CPB-p-C) with an o-nitrobenzyl group inserted between polyethylene glycol (PEG) and octadecyl ester is synthesized as an illumination-activated tumor targeting accessory for micelle-based drug carriers. The functional accessory can form a flower-like structure with folded PEC segments in aqueous solution to hide targeting biotin ligands in the core of the mixed micelle. Thus the specific binding between biotin and avidin can be suppressed by the steric hindrance of PEG shell. Upon illumination, the flower-like structure of CPB-p-C is destroyed due to the cleavage of the o-nitrobenzyl group and the biotin moieties are exposed on the surface of the micelle through the stretching process of PEG segments, generating ligand-receptor-mediated targeted delivery. By confocal laser scanning microscopy and flow cytometry, the illumination-activated, tumor-targeting delivery is studied. The influence of the amount of functional accessory in the mixed micelle on the targeting property is investigated and the optimal amount of CPB-p-C to achieve less side effects and better illumination activated tumor targeting activity is identified. The observed properties of CPB-p-C qualify it as a promising functional accessory to endow traditional drug-delivery systems with tumor selectivity.
机译:在这里,合成了一种ABA型聚合物,十八烷基-聚乙二醇(生物素)-(邻硝基苄基)-十八烷基酯(CPB-pC),其中邻硝基苄基插入聚乙二醇(PEG)和十八烷基酯之间作为照明。激活的肿瘤靶向附件,用于基于胶束的药物载体。功能性附件可以在水溶液中形成带有折叠PEC片段的花状结构,以在混合胶束的核心中隐藏靶向生物素配体。因此,可以通过PEG壳的空间位阻抑制生物素和抗生物素蛋白之间的特异性结合。照射后,由于邻硝基苄基的裂解,CPB-pC的花状结构被破坏,生物素部分通过PEG段的拉伸过程暴露在胶束表面,产生配体-受体介导的有针对性的交付。通过共聚焦激光扫描显微镜和流式细胞仪,研究了光照激活的肿瘤靶向递送。研究了混合胶束中功能性辅料的量对靶向性能的影响,并确定了CPB-p-C的最佳用量,以实现较小的副作用和更好的照明激活肿瘤靶向活性。 CPB-p-C的观察到的特性使其有希望成为功能强大的功能附件,赋予传统的药物递送系统以肿瘤选择性。

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  • 来源
    《Advanced Functional Materials》 |2014年第12期|1799-1807|共9页
  • 作者单位

    Key Laboratory of Biomedical Polymers of Ministry of Education College of Chemistry and Molecular Science Wuhan University Wuhan, 430072, China,State Key Laboratory of Chemical Engineering Department of Chemical and Biological Engineering Zhejiang University Hangzhou, 310027, China;

    Key Laboratory of Biomedical Polymers of Ministry of Education College of Chemistry and Molecular Science Wuhan University Wuhan, 430072, China;

    Key Laboratory of Biomedical Polymers of Ministry of Education College of Chemistry and Molecular Science Wuhan University Wuhan, 430072, China;

    Key Laboratory of Biomedical Polymers of Ministry of Education College of Chemistry and Molecular Science Wuhan University Wuhan, 430072, China;

    Key Laboratory of Biomedical Polymers of Ministry of Education College of Chemistry and Molecular Science Wuhan University Wuhan, 430072, China;

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