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<p>Hepatic cancer remains one of the most difficult conditions to cure, particularly when it comes to detecting and eliminating malignant metastases. To overcome hepatic cancer, various strategies have been implemented in respect to targetability and safety concern. In this study, the anticancer agent quercetin (QU) was effectively encapsulated with biocompatible polymer chitosan (CS)-hyaluronic acid (HA) to improve its poor water solubility as well as dual targetability. The resulting QU-loaded nanoparticles (QU-NPs) were formulated using CS, and HA were employed as a capping and targeting agent, and lactoferrin was added to improve drug bioavailability and targetability as well. The synthesized NPs were characterized using zeta potential analysis, particle size analysis, HR-TEM spectroscopy. The in vitro safety of QCHL-NPs was confirmed through toxicity assays on HepG2 cells. In vitro cytotoxicity data showed that QCHL-NPs required significantly lower concentrations than free QU to achieve significant inhibition 50% (IC<sub>50</sub> − 10µM in 24&#xa0;h and 1 µM in 48&#xa0;h) of proliferation of HepG2 Cells (<i>p</i> &lt; 0.01). In vivo animal study treatment with QCHL-NPs also significantly reduced antioxidant levels like TBARs (<i>p</i> &lt; 0.01) and PC (<i>p</i> &lt; 0.01) levels, while treatment with QCHL-NPs by increase caspase-3 (<i>p</i> &lt; 0.001) analysis revealed apoptosis at the molecular level. Notably, this study successfully was synthesized QU-loaded CS nanoparticles with enhanced QU loading. The final formulation, Lf-coated, HA-capped CS NPs loaded with QU (QCHL-NPs), showed the dual targetability and antitumor efficacy compared to free QU.</p>

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Formulation of Surface-Modified Quercetin-Loaded Chitosan-Hyaluronic Acid Nanoparticles for Targeted Hepatic Cancer Therapy

  • 期刊论文

  • 发表日期：

    2026年1月12日

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  • Anil Kumar Sahdev,
  • Siva Sankar Sana,
  • Priya Gupta,
  • Chandrakanta,
  • S. Saadaoui,
  • Chaitany Jayprakash Raorane,
  • Seong-Cheol Kim,
  • Anita Singh

摘要

Hepatic cancer remains one of the most difficult conditions to cure, particularly when it comes to detecting and eliminating malignant metastases. To overcome hepatic cancer, various strategies have been implemented in respect to targetability and safety concern. In this study, the anticancer agent quercetin (QU) was effectively encapsulated with biocompatible polymer chitosan (CS)-hyaluronic acid (HA) to improve its poor water solubility as well as dual targetability. The resulting QU-loaded nanoparticles (QU-NPs) were formulated using CS, and HA were employed as a capping and targeting agent, and lactoferrin was added to improve drug bioavailability and targetability as well. The synthesized NPs were characterized using zeta potential analysis, particle size analysis, HR-TEM spectroscopy. The in vitro safety of QCHL-NPs was confirmed through toxicity assays on HepG2 cells. In vitro cytotoxicity data showed that QCHL-NPs required significantly lower concentrations than free QU to achieve significant inhibition 50% (IC50 − 10µM in 24 h and 1 µM in 48 h) of proliferation of HepG2 Cells (p < 0.01). In vivo animal study treatment with QCHL-NPs also significantly reduced antioxidant levels like TBARs (p < 0.01) and PC (p < 0.01) levels, while treatment with QCHL-NPs by increase caspase-3 (p < 0.001) analysis revealed apoptosis at the molecular level. Notably, this study successfully was synthesized QU-loaded CS nanoparticles with enhanced QU loading. The final formulation, Lf-coated, HA-capped CS NPs loaded with QU (QCHL-NPs), showed the dual targetability and antitumor efficacy compared to free QU.