A quantitative MRI-based approach to estimate the permeation and retention of nanomedicines in tumors

J Control Release. 2024 Apr:368:728-739. doi: 10.1016/j.jconrel.2024.03.019. Epub 2024 Mar 19.

Abstract

Despite the potential of the enhanced permeability and retention (EPR) effect in tumor passive targeting, many nanotherapeutics have failed to produce meaningful clinical outcomes due to the variable and challenging nature of the tumor microenvironment (TME) and EPR effect. This EPR variability across tumors and inconsistent translation of nanomedicines from preclinical to clinical settings necessitates a reliable method to assess its presence in individual tumors. This study aimed to develop a reliable and non-invasive approach to estimate the EPR effect in tumors using a clinically compatible quantitative magnetic resonance imaging (qMRI) technique combined with a nano-sized MRI contrast agent. A quantitative MR imaging was developed using a dynamic contrast-enhanced (DCE) MRI protocol. Then, the permeability and retention of the nano-sized MRI contrast agent were evaluated in three different ovarian xenograft tumor models. Results showed significant differences in EPR effects among the tumor models, with tumor growth influencing the calculated parameters of permeability (Ktrans) and retention (Ve) based on Tofts pharmacokinetic (PK) modeling. Our data indicate that the developed quantitative DCE-MRI method, combined with the Tofts PK modeling, provides a robust and non-invasive approach to screen tumors for their responsiveness to nanotherapeutics. These results imply that the developed qMRI method can be beneficial for personalized cancer treatments by ensuring that nanotherapeutics are administered only to patients with tumors showing sufficient EPR levels.

Keywords: Enhanced permeability and retention effect (EPR); MRI; Magnetic resonance imaging; Nanomedicine; Nanoparticle permeation; Tofts; Tumor vasculature leakiness.

MeSH terms

  • Contrast Media* / pharmacokinetics
  • Female
  • Humans
  • Magnetic Resonance Imaging / methods
  • Models, Theoretical
  • Nanomedicine
  • Ovarian Neoplasms* / diagnostic imaging
  • Ovarian Neoplasms* / drug therapy
  • Tumor Microenvironment

Substances

  • Contrast Media