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pH protective Y1 receptor ligand functionalized antiphagocytosis BPLP-WPU micelles for enhanced tumor imaging and

Zhenqi Jiang1, Yuchen Tian2, Dingying Shan3

  • 1CAS Key Laboratory of Magnetic Materials and Devices, Key Laboratory of Additive Manufacturing Materials of Zhejiang Province, Division of Functional Materials and Nanodevices, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo 315201, China; University of Chinese Academy of Sciences, Beijing 100049, China.

Biomaterials
|April 14, 2018
PubMed

Insights

Novel Y1 receptor ligand functionalized nanoparticles with antiphagocytosis properties significantly improved breast cancer treatment outcomes, achieving a 100% survival rate and complete tumor necrosis in vivo.

Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Oncology

Background:

  • Nanoparticle drug delivery faces challenges like premature drug leakage, off-target effects, and poor tissue penetration, limiting therapeutic efficacy.
  • Previous Y1 receptor (Y1R) ligand-modified nanoparticles showed promise in breast cancer imaging but accumulated in off-target organs due to macrophage interactions.
  • Macrophages can clear nanoparticles, reducing their accumulation at the tumor site and overall therapeutic effectiveness.

Purpose of the Study:

  • To develop Y1R ligand-functionalized polymeric micelles with enhanced tumor targeting and reduced off-target accumulation.
  • To impart antiphagocytosis capability to nanoparticles by incorporating a CD47 self-peptide to evade macrophage clearance.
  • To evaluate the in vivo efficacy and biodistribution of these novel micelles for breast cancer therapy and imaging.

Main Methods:

  • Synthesis of Y1R ligand-functionalized BPLP-WPU polymeric micelles.
  • Incorporation of a CD47 human glycoprotein-based self-peptide to confer antiphagocytosis properties.
  • In vivo administration of DOX-loaded micelles for therapeutic evaluation and SPION-loaded micelles for imaging and biodistribution studies.

Main Results:

  • Self-peptide modified, DOX-loaded micelles achieved a 100% survival rate and complete tumor necrosis in vivo over 100 days.
  • In vivo imaging confirmed effective tumor targeting of SPION-loaded, self-peptide modified micelles.
  • Biodistribution analysis showed reduced particle accumulation in the liver and kidney, indicating decreased macrophage interaction, and a twofold increase in tumor accumulation.

Conclusions:

  • Y1R ligand and self-peptide co-modified BPLP-WPU micelles represent a promising strategy for targeted cancer therapy and imaging.
  • The antiphagocytosis capability significantly enhances nanoparticle accumulation at the tumor site, improving therapeutic outcomes.
  • These engineered micelles hold potential for clinical translation to improve patient survival and achieve tumor reduction.
Keywords:
AntiphagocytosisBPLP-WPUTumor imaging and therapyY(1) receptor ligandpH responsiveness

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