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Light-Triggered PEGylation/dePEGylation of the Nanocarriers for Enhanced Tumor Penetration

机译:纳米载波的光触发的聚乙二醇化/用于增强肿瘤渗透的纳米载波

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摘要

Nanocarriers-derived anticancer therapeutics typically suffers from poor tumor penetration and suboptimal antitumor efficacy. Although PEGylation improves the stability of nanoparticles and prolongs drug circulation, it further increases the size of nanoparticles and adversely affects the tumor penetration. Here, we developed a light-triggered PEGylation/dePEGylation strategy, whereby near-infrared (NIR)-/pH- dual responsive dePEGylation activates iRGD for tumor targeting. The embedded up-conversion nanoparticles (UCNPs) could efficiently convert NIR to UV-vis which cleaved the linker to remove PEG. NIR-induced dePEGylation remarkably improved vascular extravasation of drugs and deep tumor penetration. Therefore, the stimuli-responsive nanocarriers facilitated the tumor-targeted delivery of drugs through blood circulation and enhanced the antitumor effects.
机译:纳米载波衍生的抗癌治疗剂通常患有肿瘤渗透性差和次优抗肿瘤效果。 虽然聚乙二醇化改善了纳米颗粒的稳定性并延长了药物循环,但它进一步增加了纳米颗粒的尺寸,并对肿瘤渗透产生不利影响。 在这里,我们开发了一种光触发的聚乙二醇化/代苯化策略,由此近红外(NIR)/ pH - 双响应性Depynation激活IRGD用于肿瘤靶向。 嵌入式上转化纳米颗粒(UCNP)可以有效地将NIR转换为UV-VAR,其切割接头以除去PEG。 NIR诱导的Depynation显着改善了药物和深肿瘤渗透的血管外渗。 因此,刺激响应性纳米载体通过血液循环促进了肿瘤靶向递送的药物,并增强了抗肿瘤效应。

著录项

  • 来源
    《Nature reviews Cancer》 |2019年第6期|共5页
  • 作者单位

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

    Natl Univ Singapore Dept Chem Singapore 117543 Singapore;

    Chinese Acad Sci CAS Key Lab Biomed Effects Nanomat &

    Nanosafety Multidisciplinary Res Div Inst;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 肿瘤学;
  • 关键词

    Near-infrared; photocleavable; drug delivery; antitumor; drug penetration;

    机译:近红外;光致射击;药物递送;抗肿瘤;药物渗透;

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