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Updated: Dec 20, 2025

Synthesis and Characterization of Placental Chondroitin Sulfate A plCSA-Targeting Lipid-Polymer Nanoparticles
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Multifunctional Core-Shell Glyconanoparticles for Galectin-3-Targeted, Trigger-Responsive Combination Chemotherapy.

Biji Balakrishnan1, Suresh Subramanian2,3, Madhava B Mallia2,3

  • 1Nanomedicine Laboratory, Department of Biosciences and Bioengineering, IIT Bombay, Mumbai 400076, India.

Biomacromolecules
|June 3, 2020
PubMed
Summary
This summary is machine-generated.

Novel citrus pectin nanoparticles target galectin-3 (gal-3) for cancer therapy. These nanoparticles deliver drugs specifically to tumors, reduce cancer progression, and can be radiolabeled for monitoring, offering a promising platform for targeted cancer treatment.

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Biology
  • Drug Delivery

Background:

  • Galectin-3 (gal-3) is a key mediator in tumor metastasis and cancer progression.
  • Targeted drug delivery systems are needed to overcome challenges in cancer treatment.
  • Citrus pectin (CP) can be modified to create functional nanoparticles for biomedical applications.

Purpose of the Study:

  • To design galectin-3 binding core-shell glyconanoparticles from citrus pectin for targeted drug delivery.
  • To develop a system for on-demand, tumor microenvironment-responsive drug release.
  • To evaluate the efficacy of these nanoparticles in inhibiting gal-3-mediated cancer progression and drug-resistant cancer cells.

Main Methods:

  • Depolymerization of citrus pectin (CP) to create gal-3 binding dialdehyde oligomers (CPDA).
  • Fabrication of CPDA-based core-shell nanoparticles for multivalent gal-3 ligand presentation.
  • Encapsulation of sulindac (core) and doxorubicin (DOX, shell) within nanoparticles.
  • In vitro evaluation of cellular effects, drug release kinetics, and synergistic cytotoxicity.
  • Radiolabeling with Iodine-131 (¹³¹I) and in vivo biodistribution studies.

Main Results:

  • CPDA nanoparticles exhibited specific binding to galectin-3 (Kd = 160.90 μM).
  • Nanoparticles reduced cancer cell aggregation, tumor cell-endothelial cell binding, and angiogenesis.
  • Significant reduction in gal-3 expression on MDA-MB 231 cancer cells was observed.
  • On-demand drug release was achieved in response to tumor microenvironment triggers (low pH, high glucose/glutathione).
  • Drug-loaded nanoparticles showed target specificity, enhanced internalization, and synergistic cytotoxic effects, reducing IC50 by 30-fold in DOX-resistant cells.
  • Radiolabeling efficiency was ≥80%, and biodistribution studies confirmed preferential accumulation in gal-3-expressing gastric tissues.

Conclusions:

  • CPDA core-shell nanoparticles are effective platforms for galectin-3 targeting and inhibiting gal-3-mediated cancer progression.
  • The system enables triggered, target-specific drug release, enhancing efficacy against drug-resistant cancers.
  • Potential for radiolabeling offers avenues for in vivo monitoring or targeted radiotherapy.