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Design Synthesis and Characterization of pH-Sensitive PEG-PE Conjugates for Stimuli-Sensitive Pharmaceutical Nanocarriers: The Effect of Substitutes at the Hydrazone Linkage on the pH-Stability of PEG-PE Conjugates

机译：用于刺激性药物纳米载体的pH敏感PEG-PE偶联物的设计合成和表征：:连接处的取代基对PEG-PE偶联物的pH稳定性的影响

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A set of aliphatic and aromatic aldehyde-derived hydrazone(HZ)-based acid-sensitive polyethylene glycol-phosphatidylethanolamine (PEG-PE) conjugates was synthesized and evaluated for their hydrolytic stability at neutral and slightly acidic pH values. The micelles formed by aliphatic aldehyde-based PEG-HZ-PE conjugates were found to be highly sensitive to mildly acidic pH and reasonably stable at physiologic pH, while those derived from aromatic aldehydes were highly stable at both pH values. The pH-sensitive PEG-PE conjugates with controlled pH-sensitivity may find applications in biological stimuli-mediated drug targeting for building pharmaceutical nanocarriers capable of specific release of their cargo at certain pathological sites in the body (tumors, infarcts) or intracellular compartments (endosomes, cytoplasm) demonstrating decreased pH.

机译：合成了一组脂族和芳族醛衍生的（（HZ）-基酸敏感性聚乙二醇-磷脂酰乙醇胺（PEG-PE）共轭物，并评估了它们在中性和弱酸性pH值下的水解稳定性。发现由脂族醛基PEG-HZ-PE共轭物形成的胶束对弱酸性pH高度敏感，在生理pH下相当稳定，而衍生自芳族醛的胶束在两个pH值上都高度稳定。具有受控pH敏感性的pH敏感性PEG-PE共轭物可在生物刺激介导的药物靶向中找到应用，以构建能够在体内某些特定部位（肿瘤，梗塞）或细胞内区室特异性释放其货物的药物纳米载体（内体，细胞质）显示pH降低。

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期刊名称 other
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Amit A. Kale; Vladimir P. Torchilin;
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年(卷),期 -1(18),2
年度 -1
页码 363–370
总页数 23
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1. Design, Synthesis, and Characterization of pH-Sensitive PEG-PE Conjugates for Stimuli-Sensitive Pharmaceutical Nanocarriers: The Effect of Substitutes at the Hydrazone Linkage on the pH Stability of PEG-PE Conjugates [J] . Amit A. Kale, Vladimir P. Torchilin Bioconjugate Chemistry . 2007,第2期

机译：刺激性药物纳米载体的pH敏感PEG-PE偶联物的设计，合成和表征：Link键处的取代基对PEG-PE偶联物的pH稳定性的影响
2. Polyethylene glycol-phosphatidylethanolamine conjugate (PEG-PE)-based mixed micelles: some properties, loading with paclitaxel, and modulation of P-glycoprotein-mediated efflux. [J] . Dabholkar RD, Sawant RM, Mongayt DA, International Journal of Pharmaceutics . 2006,第1a2期

机译：基于聚乙二醇-磷脂酰乙醇胺共轭物（PEG-PE）的混合胶束：一些特性，紫杉醇的负载以及对P-糖蛋白介导的外排的调节。
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4. New system for effective stabilization and delivery of siRNA: Reversible siRNA-phospholipid conjugate in PEG-PE polymeric mixed micelles [C] . T. Musacchio, O. Vaze, G. DSouza, Annual meeting exposition of the Controlled Release Society . 2010

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机译：维生素E与甲氧基聚乙二醇的γ-生育三烯酚异构体的酰胺和pH可裂解的共轭物的合成理化特性和体外抗肿瘤活性
7. Design, Synthesis, and Characterization of pH-Sensitive PEG−PE Conjugates for Stimuli-Sensitive Pharmaceutical Nanocarriers: The Effect of Substitutes at the Hydrazone Linkage on the pH Stability of PEG−PE Conjugates [O] . Amit A. Kale, Vladimir P. Torchilin 2007

机译：pH敏感PEG-PE缀合物的设计，合成和表征刺激敏感药物纳米载体：替代物在腙键粘合对PEG-PE缀合物的pH稳定性的影响

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