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Preparation of mixed micelles carrying folates and stable radicals through PLA stereocomplexation for drug delivery

机译:通过PLA立体复合制备带有叶酸和稳定自由基的混合胶束以进行药物递送

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摘要

Multifunctional mixed micelles possessing targeting folates on the periphery and stable radicals in the core were prepared from the mixture of folate-poly(ethylene glycol)-block-poly(D-lactide) (FA-PEG-b-PDLA) and poly (ethylene glycol) methyl ether-block-poly(L-lactidc)- 2,2,6,6-tetramethylpiperidine-1-oxyl (mPEG-b-PLLA-TEMPO). FA-PEG-b-PDLA and mPEG-b-PLLA-TEMPO were prepared by combining ring-opening polymerization (ROP) of lactide with a series of conversion of the end functional groups. The synthesized block copolymers and their intermediates were well characterized by gel permeation chromatography (GPC) and H-1 nuclear magnetic resonance (H-1 NMR) spectroscopy. The mixture of FA-PEG-b-PDLA and mPEG-b-PLLA-TEMPO self-assembled into spherical micelles with the average diameter about 200 nm through PLA stereocomplexation, which were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM) and differential scanning calorimetry (DSC). The formed micelles were confirmed to emit electron paramagnetic resonance (EPR) signals by EPR spectroscopy. Additionally, the formed micelles exhibited high loading capacity of hydrophobic anticancer drug, controlled in vitro drug release, satisfied biocompatibility and a significantly higher cellular uptake, indicating promising applications in smart drug delivery.
机译:由叶酸-聚(乙二醇)-嵌段-聚(D-丙交酯)(FA-PEG-b-PDLA)和聚(乙烯)的混合物制备在外周具有靶向叶酸且核心具有稳定自由基的多功能混合胶束乙二醇)-甲基醚-嵌段-聚(L-内酯)-2,2,6,6-四甲基哌啶-1-氧基(mPEG-b-PLLA-TEMPO)。 FA-PEG-b-PDLA和mPEG-b-PLLA-TEMPO是通过将丙交酯的开环聚合(ROP)与一系列末端官能团的转化相结合而制备的。合成的嵌段共聚物及其中间体通过凝胶渗透色谱法(GPC)和H-1核磁共振谱(H-1 NMR)进行了很好的表征。 FA-PEG-b-PDLA和mPEG-b-PLLA-TEMPO的混合物通过PLA立体复合法自组装成平均直径约200 nm的球形胶束,其特征在于动态光散射(DLS),透射电子显微镜( TEM和差示扫描量热法(DSC)。通过EPR光谱确认形成的胶束发射电子顺磁共振(EPR)信号。另外,形成的胶束表现出高疏水性抗癌药物的负载能力,受控的体外药物释放,令人满意的生物相容性和明显更高的细胞摄取,表明在智能药物递送中有希望的应用。

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  • 来源
    《Materials science & engineering》 |2020年第3期|110464.1-110464.9|共9页
  • 作者

  • 作者单位

    Henan Normal Univ Collaborat Innovat Ctr Henan Prov Green Mfg Fine Key Lab Green Chem Media & React Minist Educ Sch Chem & Chem Engn Xinxiang 453007 Henan Peoples R China;

    Xiamen Univ Sch Pharmaceut Sci Fujian Prov Key Lab Innovat Drug Target Res Xiamen 154007 Peoples R China|Xiamen Univ Sch Pharmaceut Sci State Key Lab Cellular Stress Biol Xiamen 154007 Peoples R China;

    Henan Normal Univ Collaborat Innovat Ctr Henan Prov Green Mfg Fine Key Lab Green Chem Media & React Minist Educ Sch Chem & Chem Engn Xinxiang 453007 Henan Peoples R China|Chinese Acad Sci Key Lab Synthet & Self Assembly Chem Organ Funct 345 Lingling Rd Shanghai 200032 Peoples R China;

    ASTAR Innovis Inst Mat Res & Engn 2 Fusionopolis Way 08-03138634 Singapore 138634 Singapore;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    Stereocomplexation; Stable radical; Electron paramagnetic resonance; Drug delivery;

    机译:立体复杂化;稳定的自由基电子顺磁共振;药物输送;

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