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新颖光控Dex-H交联胶束药物释放体系的制备及协同抗肿瘤性能

Fabrication and Multi-antitumor Effect of Novel Dextran-hemin Crosslinked Micelles Triggered by Photo Conditions
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摘要 合成了一种基于血红素中双键交联的葡聚糖(Dex)载药(5-氟尿嘧啶)胶束(Dex-H交联胶束).接枝在葡聚糖上的血红素不仅可以用作光控开关控制5-氟尿嘧啶在定点部位的快速释放,而且可以同时在光照下作为光动力学疗法的光敏剂产生单线态氧,实现协同抗肿瘤作用.交联后的胶束具有良好生物相容性,同时,稳定性也相应增强,高度稀释后仍能保持稳定,有望在体内安全运输.采用3-(4,5-二甲基噻唑-2)-2,5-二甲苯基四氨唑溴盐(MTT)和荧光显微镜观察发现,激光照射下载药交联胶束表现出高效的抗癌效果,具有协同抗肿瘤作用. In order to search for novel candidate drug endowed with better antitumor activities and less neurotoxicities,a novel crosslinked dextran-hemin micelle was synthesized.Hemin grafted to dextran is not only used as a phototriggered switch for the controlled release of the loaded 5-fluorouracil(5FU) quickly,but also simultaneously as a photosensitizer for photodynamic therapy(PDT) under laser irradiation.The prepared micelles exhibit high stability against extensive dilution of solution which can restrain premature drug loss and reduce side effect to human bodies.The micelles possess good biocompatibility as well.More importantly,the 5FU loaded crosslinked dextran-hemin micelles present higher antitumor effect than those of free 5FU or crosslinked micelles under laser irradiation,indicating the excellent synergetic antitumor effect of hemin with5 FU in the as-prepared micelles.
出处 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2015年第5期1004-1011,共8页 Chemical Journal of Chinese Universities
基金 国家自然科学基金(批准号:21401001) 安徽省绿色高分子材料重点实验室开放基金资助~~
关键词 Dex-H交联胶束 5-氟尿嘧啶 单线态氧 协同抗肿瘤性能 Dextran-hemin ( Dex-H ) crosslinked micelle 5-fluorouracil Singlet oxygen Muhi-antitumoreffect
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