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    Design and evaluation of glutathione responsive glycosylated camptothecin nanosupramolecular prodrug

    Year: 2021

    Journal: Drug Deliv., Volume 28, JAN 1, page 1903–1914

    Authors: Li, Wenhua; Chen, Zhong; Liu, Xiaoying; Lian, Mingming; Peng, Haisheng; Zhang, Changmei

    Organizations: Fundamental Research Funds for the Provincial Universities of Heilongjiang Province [2017JCZX08]; Scientific Research Fund of Harbin Medical University-Daqing [DQXN201603]; Doctor groundbreaking Foundation of Harbin Medical University-Daqing [2019]; Technological Innovation Center for Precision Diagnosis and Treatment of Diseases in Cold Regions of Heilongjiang Province-Achievement Transformation and cultivation Project [CXZX-ZXKT02, CXZX-ZXKT03]

    Keywords: Glutathione; camptothecin; glycosylated; nanosupramolecular prodrug; anti-tumor ability

    A novel tumor-targeted glutathione responsive Glycosylated-Camptothecin nanosupramolecular prodrug (CPT-GL NSp) was designed and fabricated via a disulfide bond. The effects of glycoligand with different polarities on solubility, self-assembly, stability, cellular uptake, and glutathione responsive cleaving were explored, and an optimal glycosylated ligand was selected for nanosupramolecular prodrug. It has been found that CPT-GL NSp exhibited higher drug loading than traditional nanoparticles. Among of which maltose modified NSp had the strongest anti-tumor effects than that of glucose and maltotriose. CPT-SS-Maltose had a similar anti-tumor ability to Irinotecan (IR), but the superior performance in solubility, hemolysis, and uptake of HepG2 cells.
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