H₂O₂-Responsive prodrug-nanosystem based on auto-fluorescent perylenetetracarboxylic diimide hinders the foaming...

Area of Science:

• Biomedical Engineering
• Nanotechnology
• Cell Biology

Background:

• Oxidative stress contributes to various diseases.
• Oxalate bonds can neutralize excess reactive oxygen species (ROS).
• Developing targeted drug delivery systems is crucial for disease treatment.

Purpose of the Study:

• To synthesize and characterize a hydrogen peroxide (H2O2)-responsive prodrug-nanosystem.
• To evaluate the efficacy of the nanosystem in reducing oxidative stress and inflammation.
• To investigate the potential of the nanosystem in hindering foam cell progression.

Main Methods:

• Synthesis of a prodrug-nanosystem (PBI-Tre) using oxalate bonds, connecting a water-soluble drug (Tre) with a fluorescent indicator (PBI).
• Coating PBI-Tre with hyaluronic acid (HA) to create HA-PBI-Tre nanoparticles (200-300 nm size, -36.9 mV zeta potential).
• Utilizing the fluorescent properties of PBI for intracellular observation and assessing ROS levels, inflammatory factors, and lipid accumulation in RAW264.7 cells.

Main Results:

• The PBI-Tre nanoparticles exhibited a maximum fluorescence emission at 548 nm, allowing for direct cellular observation.
• HA-PBI-Tre nanoparticles demonstrated enhanced intracellular uptake and macrophage targeting.
• The nano-drug loading system effectively decreased ROS levels, inhibited inflammatory factor production, and reduced lipid accumulation in foam cells.
• These nanoparticles showed a significant inhibitory effect on foam cell progression in the RAW264.7 cell line.

Conclusions:

• A novel H2O2-responsive prodrug-nanosystem (HA-PBI-Tre) was successfully synthesized.
• The developed nanosystem effectively reduces oxidative stress, inhibits inflammation, and mitigates lipid accumulation in foam cells.
• This nanoparticle system holds promise for therapeutic strategies against diseases associated with oxidative stress and foam cell formation.