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<p>Fluorescence-based theranostic agents are gaining more attention in the fight against cancer. Herein, theranostic reagents (TA-PEG-n) consisting of a tripodal hydrophobic melphalan and different molecular weights PEG are successfully prepared. The TA-PEG-n self-assembly into nanoparticles in solution. The introduction of PEG not only transforms the tripodal center from hydrophobic to hydrophilic, but also endows it an excellent aggregation-induced emission (AIE) property. The maximum excitation wavelength can be found at 470&#xa0;nm and H<sub>2</sub>O is the solvent with the highest relative fluorescence emission intensity for the both compounds. Fluorescence of both compounds is used to track and explore cell uptake of drugs and cell distribution. The construction of the tripodal structure greatly improves the anticancer activity. The IC<sub>50</sub> to HeLa cells of TA-PEG-5000 is about 10.51 and 7.99 µmol L<sup>-1</sup>. The metabolic pathway of the TA-PEG-5000 in living organisms is also explored.</p>

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Tripodal Melphalan-PEG AIE polymer prodrug for imaging diagnostic and therapeutic cancer

  • 期刊论文

  • 发表日期：

    2025年11月19日

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  • Zheng-Hua Zhang,
  • Qian Liu,
  • You-Ming Zhang,
  • Weibing Xu,
  • Qi Lin

摘要

Fluorescence-based theranostic agents are gaining more attention in the fight against cancer. Herein, theranostic reagents (TA-PEG-n) consisting of a tripodal hydrophobic melphalan and different molecular weights PEG are successfully prepared. The TA-PEG-n self-assembly into nanoparticles in solution. The introduction of PEG not only transforms the tripodal center from hydrophobic to hydrophilic, but also endows it an excellent aggregation-induced emission (AIE) property. The maximum excitation wavelength can be found at 470 nm and H2O is the solvent with the highest relative fluorescence emission intensity for the both compounds. Fluorescence of both compounds is used to track and explore cell uptake of drugs and cell distribution. The construction of the tripodal structure greatly improves the anticancer activity. The IC50 to HeLa cells of TA-PEG-5000 is about 10.51 and 7.99 µmol L-1. The metabolic pathway of the TA-PEG-5000 in living organisms is also explored.