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首页> 外文期刊>ACS applied materials & interfaces >Redox-Responsive Self-Assembly Micelles from Poly(N-acryloylmorpholine-block-2-acryloyloxyethyl ferrocenecarboxylate) Amphiphilic Block Copolymers as Drug Release Carriers
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Redox-Responsive Self-Assembly Micelles from Poly(N-acryloylmorpholine-block-2-acryloyloxyethyl ferrocenecarboxylate) Amphiphilic Block Copolymers as Drug Release Carriers

机译:来自聚(N-丙烯酰基卟啉 - 嵌段-2-丙烯酰氧基甲基铁核羧酸盐)两亲嵌段共聚物的氧化还原响应的自组装胶束作为药物释放载体

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摘要

Novel well-defined redox-responsive ferrocene-containing amphiphilic block copolymers (PACMO-b-PAEFC) were synthesized by ATRP, with poly(N-acryloylmorpholine) (PACMO) as hydrophilic blocks and poly(2-acryloyloxyethyl ferrocenecarboxylate) (PAEFC) as hydrophobic blocks. The copolymers were characterized by FT-IR and H-1 NMR spectroscopies and gel permeation chromatography, and the crystalline behavior was determined by X-ray diffraction and small-angle X-ray scattering. The results showed that the size of the lamellar crystals and crystallinity vary with the systematic compositions while the periodic structure of the lamellar stacks has no obvious change. These block copolymers could self-assemble and form globular nanoscaled coreshell micellar aggregates in aqueous solution. The reductive ferrocene groups could be changed into hydrophilic ferrocenium via mild oxidation, whereas the polymer micelles at the oxidation state could reversibly recover from their original states upon reduction by vitamin C. The tunable redox response was investigated and verified by transmission electron microscopy, ultravioletvisible spectroscopy, cyclic voltammetry, and dynamic light scattering measurements. The copolymer micelles were used to entrap anticancer drug paclitaxel (PTX), with high drug encapsulation efficiency of 61.4%, while the PTX-loaded drug formulation exhibited oxidation-controlled drug release, and the release rate could be mediated by the kinds and concentrations of oxidants. MTT assay was performed to disclose the biocompatibility and security of the copolymer micelles and to assess anticancer efficiency of the PTX-loaded nanomicelles. The developed copolymer nanomicelles with reversible redox response are anticipated to have potential in targeted drug delivery systems for cancer therapy.
机译:通过ATRP合成新颖的含氧化还原浓度的两亲嵌段共聚物(PACMO-B-PAEFC),用聚(N-丙烯酰上卟啉)(PACMO)作为亲水嵌段和聚(2-丙烯酰氧基乙基铁羧酸羧酸甲酯)(PHEFC)作为疏水块。通过FT-IR和H-1 NMR谱和凝胶渗透色谱法表征共聚物,并通过X射线衍射和小角度X射线散射测定结晶行为。结果表明,层状晶体和结晶度的尺寸随系统组合物而变化,而层状堆的周期性结构没有明显的变化。这些嵌段共聚物可以在水溶液中自组装并形成球状纳米级CoreShell胶束聚集体。可通过温和的氧化将还原二茂铁基团变成亲水性氧化锰,而氧化状态的聚合物胶束可以在维生素C的减少后从原始状态可逆地恢复。通过透射电子显微镜,紫外线光谱检查进行调节氧化还原响应和验证,循环伏安法和动态光散射测量。共聚物胶束用于诱捕抗癌药物紫杉醇(PTX),具有高药物包封效率为61.4%,而PTX负载的药物制剂表现出氧化控制的药物释放,并且释放速率可以通过种类和浓度介导氧化剂。进行MTT测定以公开共聚物胶束的生物相容性和安全性,并评估PTX负载的纳米钙的抗癌效率。通过可逆氧化还原反应的开发的共聚物纳米细胞预计具有癌症治疗的靶向药物递送系统的潜力。

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