Dual-Drug Nanomedicine Assembly with Synergistic Anti-Aneurysmal Effects via Inflammation Suppression and Extracellular Matrix Stabilization

Small. 2024 Oct;20(43):e2402141. doi: 10.1002/smll.202402141. Epub 2024 Jul 2.

Abstract

Abdominal aortic aneurysm (AAA) represents a critical cardiovascular condition characterized by localized dilation of the abdominal aorta, carrying a significant risk of rupture and mortality. Current treatment options are limited, necessitating novel therapeutic approaches. This study investigates the potential of a pioneering nanodrug delivery system, RAP@PFB, in mitigating AAA progression. RAP@PFB integrates pentagalloyl glucose (PGG) and rapamycin (RAP) within a metal-organic-framework (MOF) structure through a facile assembly process, ensuring remarkable drug loading capacity and colloidal stability. The synergistic effects of PGG, a polyphenolic antioxidant, and RAP, an mTOR inhibitor, collectively regulate key players in AAA pathogenesis, such as macrophages and smooth muscle cells (SMCs). In macrophages, RAP@PFB efficiently scavenges various free radicals, suppresses inflammation, and promotes M1-to-M2 phenotype repolarization. In SMCs, it inhibits apoptosis and calcification, thereby stabilizing the extracellular matrix and reducing the risk of AAA rupture. Administered intravenously, RAP@PFB exhibits effective accumulation at the AAA site, demonstrating robust efficacy in reducing AAA progression through multiple mechanisms. Moreover, RAP@PFB demonstrates favorable biosafety profiles, supporting its potential translation into clinical applications for AAA therapy.

Keywords: abdominal aortic aneurysm; metal–organic framework; nanodrug delivery system; pentagalloyl glucose; rapamycin.

MeSH terms

  • Animals
  • Aortic Aneurysm, Abdominal* / drug therapy
  • Aortic Aneurysm, Abdominal* / metabolism
  • Aortic Aneurysm, Abdominal* / pathology
  • Drug Synergism
  • Extracellular Matrix* / metabolism
  • Humans
  • Hydrolyzable Tannins
  • Inflammation* / drug therapy
  • Inflammation* / pathology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Metal-Organic Frameworks / chemistry
  • Mice
  • Myocytes, Smooth Muscle / drug effects
  • Myocytes, Smooth Muscle / metabolism
  • Nanomedicine* / methods
  • RAW 264.7 Cells
  • Sirolimus* / chemistry
  • Sirolimus* / pharmacology

Substances

  • Sirolimus
  • pentagalloylglucose
  • Metal-Organic Frameworks
  • Hydrolyzable Tannins