基于柱[5]芳烃的超分子嵌段两亲聚合物的癌症靶向药物运输体系
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摘要
基于水溶性柱[5]芳烃和紫精之间的主客体分子识别构筑两亲超分子刷共聚物。超分子共聚物自组装成纳米颗粒,利用其聚集诱导发光效应的优点作为自成像的药物递送载体。抗癌药物阿霉素的封装引起四苯乙烯和DOX生色团两者的荧光失活,这是由于能量转移中继效应,通过荧光共振能量转移和聚集诱导淬灭介导。装载DOX分子的释放可以通过低pH值和还原酶触发,由于ETR效应消失,淬灭的荧光恢复,通过观察能量转移的位置和荧光的强度变化以实现药物释放过程中的原位可视化。装载DOX的超分子纳米颗粒表面上具有生物素配体作为靶向试剂,从而可优先进攻DOX生物素受体过度表达的癌细胞。体外研究表明,通过超分子纳米材料装载的阿霉素,对癌细胞具有比正常细胞更高的选择性毒性。
The first pillararene-based amphiphilic supramolecular brush copolymer(P5-PEG-BiotinéPTPE) was constructed on the basis of the host–guest molecular recognition between a water-soluble pillar[5]arene(P5) and a viologen salt(C_5V). P5-PEG-BiotinéPTPE self-assembled into nanoparticles, which were utilized as a self-imaging drug delivery vehicle. Encapsulation of anticancer drug doxorubicin(DOX) caused deactivation of the fluorescences of both the tetraphenylethene(TPE)and DOX chromophores. The release of loaded DOX molecules can be triggered by low pH and reductase, recovering the "silenced" fluorescence, achieving in situ visualization of the drug release process by observing the location and magnitude of the energy transfer-dependent fluorescence variation.
引文
[1]Peer,D.;Karp,J.M.;Hong,S.;Farokhzad,O.C.;Margalit,R.;Langer,R.Nat.Nanotech.2007,2,751.

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