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A supramolecular diagnosis and treatment integrated agent: synthesis and self-assembly of stimulus-responsive star-shaped copolymer
European Polymer Journal ( IF 5.8 ) Pub Date : 2020-07-01 , DOI: 10.1016/j.eurpolymj.2020.109833
Mi Zhou , Feng Ling , Jie Li

Abstract We now report a star-shaped supramolecular copolymer for diagnosis and treatment by chelated with Gd3+ ion as magnetic resonance imaging (MRI) contrast agent and drug-carried for controlling release agent. The copolymer is prepared by the host-guest inclusion complexation between the host polymer polycaprolactone-β-cyclodextrin (4sPCL-CD) and the guest polymer adamantylamine-poly-L-lactic-block-poly(N-isopropylacrylamide-co-2-hydroxyethylmethacrylate-diethylenetriamine penta acetic acid) (AD-PLLA-b-P(NIPAM-co-HEMA-DTPA)) and can self-assemble into spherical micelles in aqueous solution. By adding 2-adamantylamine hydrochloride (AD-NH2), the supramolecular copolymer can be disassembled to the host and guest polymers and its molecular weight will be decreased. When the polymeric micelles are chelated with Gd3+ ion, they exhibit T1 relaxivity as a kind of contrast agent for MRI. This contrast agent can maintain a large molecular size to stay in vivo and also can reduce its molecular size quickly and metabolize rapidly from the body by disassembled. Also, as the copolymer carries drugs, it displays burst release and thermal-response release behaviors, due to its dis-assembly and thermal-response PNIPAM chain respectively. Thus, the supramolecular copolymer from the host-guest inclusion complexation is expected to realize diagnosis and treatment feature for clinic.

中文翻译:

一种超分子诊疗一体化药剂:刺激响应星形共聚物的合成与自组装

摘要 我们现在报道了一种星形超分子共聚物,通过螯合Gd3+离子作为磁共振成像(MRI)造影剂和载药控释剂用于诊断和治疗。该共聚物是通过主体聚合物聚己内酯-β-环糊精(4sPCL-CD)和客体聚合物金刚胺-聚-L-乳酸-嵌段-聚(N-异丙基丙烯酰胺-co-2-羟乙基甲基丙烯酸酯)之间的主客体包合物制备的-二亚乙基三胺五乙酸)(AD-PLLA-bP(NIPAM-co-HEMA-DTPA))并且可以在水溶液中自组装成球形胶束。通过加入2-金刚胺盐酸盐(AD-NH2),超分子共聚物可以分解为主体和客体聚合物,并降低其分子量。当聚合物胶束与 Gd3+ 离子螯合时,它们表现出 T1 弛豫性,作为 MRI 的一种造影剂。这种造影剂可以保持较大的分子大小以留在体内,也可以快速缩小其分子大小并通过分解从体内快速代谢。此外,当共聚物携带药物时,由于其分解和热响应 PNIPAM 链,它表现出突释和热响应释放行为。因此,来自主客体包合络合的超分子共聚物有望实现临床诊断和治疗功能。由于其分解和热响应 PNIPAM 链,它分别显示了爆发释放和热响应释放行为。因此,来自主客体包合络合的超分子共聚物有望实现临床诊断和治疗功能。由于其分解和热响应 PNIPAM 链,它分别显示了爆发释放和热响应释放行为。因此,来自主客体包合络合的超分子共聚物有望实现临床诊断和治疗功能。
更新日期:2020-07-01
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