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

Oshra Betzer, Malka Shilo, Renana Opochinsky, Eran Barnoy, Menachem Motiei, Eitan Okun, Gal Yadid, Rachela Popovtzer*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
Pages (from-to)1533-1546
Number of pages14
Issue number13
StatePublished - Jul 2017
Externally publishedYes


  • blood-brain barrier
  • computed tomography
  • drug delivery
  • gold nanoparticles
  • insulin
  • nanoparticle size


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