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Reduction-Degradable Shell Cross-Linked Micelle with PH-Responsive Cores Prepared via Click Chemistry

机译:可通过点击化学制备的可减少可降解的壳体交联胶束,用pH-响应芯

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A well-defined poly[(ethylene glycol)-block-2-(dimethylamino)ethyl methacrylate -block-2-(diethylamino) methacrylate] (PEG-b-DMA-b-DEA) triblock copolymer was synthesized via atom transfer radical polymerization (ATRP) by successively polymerization of DMA and DEA monomers using a PEG-based macroinitiator, and obtained copolymer was then converted to be PEG-b-P(DMA-co-QDMA)-b-PDEA copolymer with "clickable" moieties in the middle block by the quaternization with propargyl bromide. Those copolymers prepared were characterized by proton Nuclear Magnetic Resonance (~1H NMR) and Gel Permeation Chromatography (GPC), and its self-assembly behavior and subsequently fixation with bis-(azidoethyl)disulfide via click chemistry resulting reduction-sensitive shell-cross-linked (SCL) micelle in purely aqueous solution were investigated by Transmission Electron Microscopy (TEM) and Dynamic Light Scattering (DLS). The results show the micellar structure could be effectively cross-linked via click chemistry and also be dissociated at reduction condition, which may realize it's potential application as novel drug delivery carriers.
机译:一个定义明确的聚[(乙二醇) - 嵌段 - 2-(二甲基氨基)乙基甲基丙烯酸酯 - 嵌段 - 2-(二乙基氨基)甲基丙烯酸酯](PEG-B-DMA-B-DEA)三嵌段经原子转移自由基聚合合成的共聚物然后(ATRP)通过使用基于PEG的大分子引发剂DMA和DEA的单体的聚合连续地,和得到的共聚物转化为PEG-BP(DMA - 共 - QDMA) - 嵌段 - 共聚物PDEA在中间块“可点击的”部分通过与炔丙基溴的季铵化。制备的那些共聚物的特征在于通过质子核磁共振(〜1H NMR)和凝胶渗透色谱(GPC),其自组装行为,并随后固定用双 - (叠氮基乙基)二硫化物经由点击化学所得还原敏感的壳的横在纯水溶液联(SCL)胶束是由透射电子显微镜(TEM)和动态光散射(DLS)分析。结果表明,胶束结构可以有效交联通过点击化学以及在还原条件下解离,这可以实现它的潜在应用作为新型药物传递载体。

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