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Related Experiment Video

Updated: Feb 5, 2026

Microwave-assisted Functionalization of Polyethylene glycol and On-resin Peptides for Use in Chain Polymerizations and Hydrogel Formation
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Peptide-Functionalized Hydrogel Cubes for Active Tumor Cell Targeting.

Bing Xue, Veronika Kozlovskaya, Mohammad Asif Sherwani

  • 1Southern Research , Birmingham , Alabama 35205 , United States.

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|September 1, 2018
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Summary

Researchers created targeted hydrogel particles that specifically deliver anticancer drugs to cancer cells. Smaller, peptide-modified particles showed enhanced uptake by tumor cells, improving targeted drug delivery strategies.

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Drug Delivery

Background:

  • Targeted drug delivery systems enhance therapeutic efficiency by conjugating bioactive molecules to nano- or micrometer-sized carriers.
  • Developing stimuli-responsive drug carriers is crucial for controlled drug release at the tumor site.

Purpose of the Study:

  • To engineer pH- and redox-sensitive hydrogel particles with a cancer cell-targeting ligand for specific tumor targeting.
  • To investigate the controlled release of doxorubicin from these targeted hydrogel particles.
  • To evaluate the impact of particle size and targeting ligand on cancer cell internalization.

Main Methods:

  • Fabrication of poly(methacrylic acid) (PMAA) hydrogel cubes (700 nm and 2 μm) using sacrificial templates.
  • Surface conjugation of a hepsin-targeting peptide (IPLVVPL) to disulfide-stabilized hydrogels via thiol-amine reaction.
  • Assessment of hydrogel properties (structural integrity, stability, sensitivity) post-conjugation.
  • Evaluation of cell uptake kinetics and selectivity in hepsin-positive (MCF-7, SK-OV-3) and hepsin-negative (PC-3) cancer cell lines.

Main Results:

  • Peptide conjugation did not compromise hydrogel integrity, stability, or stimuli-responsiveness.
  • Smaller (700 nm) peptide-conjugated hydrogels showed significantly enhanced uptake in hepsin-positive MCF-7 cells compared to non-targeted or larger hydrogels.
  • A 3-10 fold higher particle internalization was observed in hepsin-positive cells (MCF-7, SK-OV-3) versus hepsin-negative cells (PC-3), confirming targeting selectivity.
  • Cellular uptake was dependent on cell type and hydrogel size, highlighting the importance of ligand-receptor interactions.

Conclusions:

  • A facile method for creating enhanced tumor-targeting carriers of submicrometer size was developed.
  • Particle size and surface modification with targeting ligands are critical parameters for optimizing targeted drug delivery.
  • These targeted hydrogel particles show promise for improving the specificity and efficacy of anticancer drug delivery.