A polymeric micelle magnetic resonance imaging (MRI) contrast agent reveals blood-brain barrier (BBB) permeability for macromolecules in cerebral ischemia-reperfusion injury

J Control Release. 2017 May 10:253:165-171. doi: 10.1016/j.jconrel.2017.03.020. Epub 2017 Mar 18.

Abstract

Blood-brain barrier (BBB) opening is a key phenomenon for understanding ischemia-reperfusion injuries that are directly linked to hemorrhagic transformation. The recombinant human tissue-type plasminogen activator (rtPA) increases the risk of symptomatic intracranial hemorrhages. Recent imaging technologies have advanced our understanding of pathological BBB disorders; however, an ongoing challenge in the pre-"rtPA treatment" stage is the task of developing a rigorous method for hemorrhage-risk assessments. Therefore, we examined a novel method for assessment of rtPA-extravasation through a hyper-permeable BBB. To examine the image diagnosis of rtPA-extravasation for a rat transient occlusion-reperfusion model, in this study we used a polymeric micelle MRI contrast-agent (Gd-micelles). Specifically, we used two MRI contrast agents at 1h after reperfusion. Gd-micelles provided very clear contrast images in 15.5±10.3% of the ischemic hemisphere at 30min after i.v. injection, whereas a classic gadolinium chelate MRI contrast agent provided no satisfactorily clear images. The obtained images indicate both the hyper-permeable BBB area for macromolecules and the distribution area of macromolecules in the ischemic hemisphere. Owing to their large molecular weight, Gd-micelles remained in the ischemic hemisphere through the hyper-permeable BBB. Our results indicate the feasibility of a novel clinical diagnosis for evaluating rtPA-related hemorrhage risks.

Keywords: A polymeric micelle MRI contrast agent; Blood–brain barrier (BBB) permeability; Drug targeting; Focal ischemia-reperfusion injury; Magnetic resonance imaging (MRI).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood-Brain Barrier / metabolism*
  • Contrast Media* / administration & dosage
  • Contrast Media* / pharmacokinetics
  • Gadolinium DTPA* / administration & dosage
  • Gadolinium DTPA* / pharmacokinetics
  • Gadolinium* / administration & dosage
  • Gadolinium* / pharmacokinetics
  • Infarction, Middle Cerebral Artery / diagnostic imaging
  • Infarction, Middle Cerebral Artery / metabolism*
  • Magnetic Resonance Imaging
  • Male
  • Micelles*
  • Permeability
  • Polymers / administration & dosage
  • Polymers / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Reperfusion Injury / diagnostic imaging
  • Reperfusion Injury / metabolism*

Substances

  • Contrast Media
  • Micelles
  • Polymers
  • Gadolinium
  • Gadolinium DTPA