The effect of nanoparticle size on the ability to cross the blood-brain barrier: an in vivo study

Nanomedicine (Lond). 2017 Jul;12(13):1533-1546. doi: 10.2217/nnm-2017-0022. Epub 2017 Jun 16.

Abstract

Aim: Our goal was to develop an efficient nanoparticle-based system that can overcome the restrictive mechanism of the blood-brain barrier (BBB) by targeting insulin receptors and would thus enable drug delivery to the brain.

Methods: Insulin-coated gold nanoparticles (INS-GNPs) were synthesized to serve as a BBB transport system. The effect of nanoparticle size (20, 50 and 70 nm) on their ability to cross the BBB was quantitatively investigated in Balb/C mice.

Results: The most widespread biodistribution and highest accumulation within the brain were observed using 20 nm INS-GNPs, 2 h post injection. In vivo CT imaging revealed that particles migrated to specific brain regions, which are involved in neurodegenerative and neuropsychiatric disorders.

Conclusion: These findings promote the optimization of nanovehicles for transport of drugs through the BBB. The insulin coating of the particles enabled targeting of specific brain regions, suggesting the potential use of INS-GNPs for delivery of various treatments for brain-related disorders.

Keywords: blood–brain barrier; computed tomography; drug delivery; gold nanoparticles; insulin; nanoparticle size.

MeSH terms

  • Animals
  • Biological Transport
  • Blood-Brain Barrier / metabolism*
  • Contrast Media
  • Drug Delivery Systems
  • Gold*
  • Humans
  • Insulin / chemistry*
  • Iopamidol
  • Metal Nanoparticles / chemistry*
  • Mice
  • Mice, Inbred BALB C
  • Molecular Targeted Therapy
  • Optical Imaging
  • Particle Size
  • Surface Properties
  • Tissue Distribution
  • Tomography Scanners, X-Ray Computed

Substances

  • Contrast Media
  • Insulin
  • Gold
  • Iopamidol