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Preparation and characterization of pH and thermally responsive perfluoropolyether acrylate copolymer micelles and investigation its drug‐loading properties

机译:pH值和热响应性全氟聚醚丙烯酸酯共聚物胶束的制备和表征及其载药性能研究

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摘要

Abstract In this study, pH and thermally responsive P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480) was prepared by atom transfer radical polymerization (ATRP) using perfluoropolyether hydroxyethyl methacrylate (PFPHM) as hydrophobic core, 2‐(Dimethylamino) ethyl methacrylate as pH and thermal response function segment, and poly (ethylene glycol) methyl ether acrylate480 as hydrophilic shell, respectively. The chemical structure, critical micelle concentration (CMC), lower critical solution temperature (LCST), biological toxicity, stability of micelles, drug‐loading performance and cumulative drug release rate of prepared P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480) were analyzed by 19F NMR, 1H NMR, FTIR, DLS, UV–Vis, laser confocal microscopy and fluorescence spectrophotometer. The results show that P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480) exhibites a CMC of 7.5 g/L, LCST of 37.6°C and excellent micelle stability. Moreover, the analysis of drug‐loading indicates that the polymer displayed drug loading efficiency (DL) is 21.3 and the encapsulation efficiency (EE) is 90.0. Its cumulative drug release rates at pH = 6.5 (42°C) is almost double of those at pH = 7.4 (42°C), pH = 6.5 (37°C) and pH = 7.4 (37°C). These results suggeste that the P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480) at pH ranging from 6.5 to 7.4 and temperature ranging from 37 to 42°C are pH and temperature sensitive. It has great potential application as a drug loading for DOX.
机译:摘要 以全氟聚醚甲基丙烯酸羟乙酯(PFPHM)为疏水核心,甲基丙烯酸二甲氨基乙酯2-(二甲氨基)乙酯为pH值和热响应函数段,聚乙二醇甲醚丙烯酸酯480为亲水壳,采用原子转移自由基聚合(ATRP)法制备了pH值和热响应性P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480)。采用19F NMR、1H NMR、FTIR、DLS、紫外-可见分光光度计、激光共聚焦显微镜和荧光分光光度计等手段分析了制备的P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480)的化学结构、临界胶束浓度(CMC)、临界溶液温度(LCST)、生物毒性、胶束稳定性、载药性能及累积药物释放速率。结果表明,P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480)表现出7.5 g/L的CMC,LCST为37.6°C,胶束稳定性优异。此外,载药量分析表明,聚合物的载药效率(DL)为21.3%,包封效率(EE)为90.0%。在pH = 6.5 (42°C) 时,其累积药物释放速率几乎是 pH = 7.4 (42°C)、pH = 6.5 (37°C) 和 pH = 7.4 (37°C) 时的两倍。这些结果表明,在pH范围为6.5至7.4,温度范围为37至42°C时,P(PFPHM9‐b‐DMAEMA‐b‐PEGMEA480)对pH和温度敏感。它作为DOX的载药量具有很大的应用潜力。

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