Phosphatidylserine-microbubble targeting-activated microglia/macrophage in inflammation combined with ultrasound for breaking through the blood-brain barrier

J Neuroinflammation. 2018 Nov 30;15(1):334. doi: 10.1186/s12974-018-1368-1.

Abstract

Background and purpose: Inflammatory reaction plays a crucial role in cerebral ischemia reperfusion (IR) injury. It has been shown that activated microglia long-term existed in cerebral ischemia and induced second injury. Therefore, we hypothesize that prepared phosphatidylserine (PS)-modified microbubbles (PS-MBs) combined with ultrasound-targeted microbubble destruction (UTMD) can safely open the blood-brain barrier (BBB) and target activated microglia for inflammatory area in the later stage of ischemia reperfusion.

Methods: To verify our hypothesis, rat model of IR was established, then the change of activated microglia/macrophage (M/M) and permeability of BBB at 1, 7, 14, and 21 days could be clearly observed post IR. And the activated M/M still can be observed during the whole experiment.

Results: The Evans blue extravasation of BBB gradually declined from day 1 to day 21. Compared to the control group, microbubbles containing PS were taken up more by activated M/M (approximately twofold) both in vitro and in vivo.

Conclusions: PS-MBs combined with ultrasound (US) exposure could safely open BBB, and the resulting PS nanoparticles (PS-NPs) could further target activated M/M in the neuroinflammation.

Keywords: Blood–brain barrier; Ischemia; Microbubbles; Phosphatidylserine; Ultrasound-targeted microbubble destruction.

MeSH terms

  • Animals
  • Blood-Brain Barrier / pathology*
  • Cerebral Infarction / etiology
  • Cerebral Infarction / pathology
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Encephalitis* / diagnostic imaging
  • Encephalitis* / etiology
  • Encephalitis* / pathology
  • Hypoxia-Ischemia, Brain / complications*
  • Macrophages / physiology
  • Magnetic Resonance Imaging
  • Male
  • Microbubbles / therapeutic use*
  • Microglia / physiology
  • Permeability
  • Phosphatidylserines / therapeutic use*
  • Rats
  • Rats, Sprague-Dawley
  • Sincalide / metabolism
  • Time Factors
  • Ultrasonography / adverse effects*

Substances

  • Phosphatidylserines
  • Sincalide