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Synthesis of Monocyte-targeting Peptide Amphiphile Micelles for Imaging of Atherosclerosis
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Inflammatory endothelium-targeted and cathepsin responsive nanoparticles are effective against atherosclerosis

Fei Fang1,2, Yinghao Ni1, Hongchi Yu1

  • 1Institute of Biomedical Engineering, West China School of Basic Medical Sciences & Forensic Medicine, Sichuan University, Chengdu 610041, China.

Theranostics
|June 8, 2022
PubMed

Insights

New nanoparticles deliver rapamycin (RAP) effectively for atherosclerosis treatment. These targeted and responsive nanoparticles (T/R NPs) reduce inflammation and block plaque development in mice.

Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Cardiovascular Research

Background:

  • Atherosclerosis involves lipid accumulation and plaque formation, posing challenges for pharmacological treatments due to issues with drug delivery and clearance.
  • Current therapies for atherosclerosis struggle with targeted delivery, controlled release, and preventing non-specific clearance of drugs.

Purpose of the Study:

  • To develop an integrin αvβ3-targeted and cathepsin K (CTSK)-responsive nanoparticle system for localized rapamycin (RAP) delivery.
  • To overcome the limitations of current atherosclerosis treatments by enhancing drug targeting and controlled release.

Main Methods:

  • Engineered targeted and responsive nanoparticles (T/R NPs) using PLGA-PEG-c(RGDfC) and CTSK-sensitive PLGA-Pep-PEG polymers.
  • Incorporated a FRET probe into PLGA-Pep-PEG to monitor CTSK-mediated hydrolysis events.
  • Evaluated RAP@T/R NPs in vitro for drug release and effects on macrophages, and in vivo in ApoE-/- mice for atherosclerosis progression and inflammation.

Main Results:

  • RAP@T/R NPs demonstrated CTSK-stimulated accelerated RAP release in vitro, inhibiting macrophage phagocytosis of oxidized LDL (OxLDL) and cytokine release.
  • T/R NPs exhibited prolonged blood circulation and enhanced accumulation in atherosclerotic lesions at both early and late stages.
  • Treatment with RAP@T/R NPs significantly inhibited atherosclerosis development and reduced systemic and local inflammation in ApoE-/- mice.

Conclusions:

  • Targeted and responsive nanoparticles (T/R NPs) show promise for localized rapamycin delivery in atherosclerosis therapy.
  • This novel drug delivery system offers a safer and more efficient therapeutic strategy for atherosclerosis.
  • The CTSK-responsive nature of the nanoparticles enables precise drug release at lesion sites, improving treatment efficacy.

Keywords:
atherosclerosiscathepsin kdrug deliverynanoparticlesrapamycin

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