Effective Oxidation-Responsive Polyester Nanocarriers for Anti-Inflammatory Drug Delivery.

Area of Science:

• Biomaterials Science
• Polymer Chemistry
• Nanotechnology

Background:

• Inflammatory diseases are linked to high oxidant levels (ROS/RNS).
• Targeted drug delivery systems can improve anti-inflammatory therapy efficacy.
• Oxidation-responsive systems offer selective drug release at inflammatory sites, reducing side effects.

Purpose of the Study:

• To evaluate an oxidation-sensitive PEGylated alternating polyester (mPEG-b-P(PA-alt-GPBAe)) as a nanocarrier.
• To investigate the potential of this nanocarrier for delivering curcumin (CUR) in anti-inflammatory therapy.

Main Methods:

• Copolymers synthesized via click reaction and ring-opening polymerization.
• Curcumin loaded into nanoparticles (NPs-CUR) through self-assembly.
• In vitro studies included drug release, cytotoxicity, cellular uptake, and anti-inflammatory effects in LPS-stimulated macrophages.
• In vivo studies assessed anti-inflammatory effects in a murine ankle inflammation model.

Main Results:

• NPs-CUR demonstrated rapid curcumin release in response to hydrogen peroxide (H2O2).
• NPs-CUR significantly inhibited pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) and increased IL-10 in activated macrophages.
• Local injection of NPs-CUR suppressed acute ankle inflammation in mice and reduced pro-inflammatory cytokine expression.

Conclusions:

• The developed oxidation-responsive polymeric nanoparticles show promise as effective drug delivery systems.
• Both in vitro and in vivo results support their potential for anti-inflammatory therapy.