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Well-defined pH-responsive triblock glycopolymer architectures for controlled loading and release doxorubicin

机译:定义的pH响应性三嵌段糖煤结构,用于控制加载和释放多柔比星

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To explore drug loading and release behavior of pH-responsive block glycopolymers used as an anticancer drug delivery carriers, poly(ethylene glycol)-b-poly(2-(diethylamino) ethyl methacrylate)-b-poly(2-gluconamidoethyl methacrylate) (PEG1_(13)-b-PDEA_(41)-b-PGAMA_(34)), was synthesized via Atom Transfer Radical Polymerization (ATRP) by polymerized poly (2-gluconamidoethyl methacrylate) (GAMA) and 2-(diethylamino) ethyl methacrylate (DEA) monomers using a poly(ethylene glycol)-based (PEG-based) macroinitiator without protecting group chemistry. proton nuclear magnetic resonance ('H NMR) and Gel Permeation Chromatography (GPC) were used to characterize their structures, their self-assembly behaviors and drug loading and release behavior of Doxorubicin (DOX) as the model of an anticancer drug were further investigated in detailed by Transmission Electron Microscopy (TEM), zeta-potential, and ultraviolet-visible spectrophotometer (UV-Vis). The results show glycopolymers self-assembly into micelles at basic conditions and dissociate to be unimers at acidic conditions, this pH-responsiveness endows block glycopolymer to possess the ability to load the DOX at physiological condition (pH 7.4) and smart release at mimicking tumor acidic environments (pH 5.5), however, the glycopolymer at pH 5.5 Phosphate Buffered Saline (PBS) released medium possesses faster drug release profile compared with the released medium at pH 7.4 PBS. This study provides a promising light for designing novel drug delivery carrier for potential applications in cancer chemotherapy.
机译:为了探索用作抗癌药物输送载体的pH响应嵌段糖聚合物的药物载荷和释放行为,聚(乙二醇)-b-聚(2-(二乙基氨基)甲基丙烯酸乙酯)-B-聚(2-葡糖氨基甲基丙烯酸甲酯)(通过聚合的聚(2-葡糖氨基甲基丙烯酸甲酯)(GAMA)和2-(二乙基氨基)甲基丙烯酸乙酯,通过原子传递自由基聚合(ATRP)合成PEG1_(13)-B-PGAMA_(34))通过原子转移自由基聚合(ATRP)合成(DEA)使用聚(基于乙二醇)的单体(基于PEG的)大型缺发剂而不保护群化学。质子核磁共振('H NMR)和凝胶渗透色谱(GPC)用于表征其结构,其自组装行为和药物载荷和多柔比星(DOX)的释放行为作为抗癌药的模型进行了进一步研究通过透射电子显微镜(TEM),Zeta电位和紫外线可见光光度计(UV-VI)进行详细描述。结果显示甘甘油聚合物在基本条件下将胶束自组装成胶束,并在酸性条件下解离是百分比的,该pH-反应性赋予颗粒甘油共聚物,以具有在生理条件(pH7.4)下装载DOX的能力,并在模拟肿瘤酸性时智能释放能力然而,环境(pH 5.5),pH5.5磷酸盐缓冲盐水(PBS)释放培养基的甘油聚合物与pH 7.4 PBS的释放介质相比具有更快的药物释放曲线。本研究提供了用于设计新药递送载体的有希望的灯,用于癌症化疗中的潜在应用。

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