Targeting of nanoparticles to the cerebral vasculature after traumatic brain injury

PLoS One. 2024 Jun 10;19(6):e0297451. doi: 10.1371/journal.pone.0297451. eCollection 2024.

Abstract

Traumatic brain injury has faced numerous challenges in drug development, primarily due to the difficulty of effectively delivering drugs to the brain. However, there is a potential solution in targeted drug delivery methods involving antibody-drug conjugates or nanocarriers conjugated with targeting antibodies. Following a TBI, the blood-brain barrier (BBB) becomes permeable, which can last for years and allow the leakage of harmful plasma proteins. Consequently, an appealing approach for TBI treatment involves using drug delivery systems that utilize targeting antibodies and nanocarriers to help restore BBB integrity. In our investigation of this strategy, we examined the efficacy of free antibodies and nanocarriers targeting a specific endothelial surface marker called vascular cell adhesion molecule-1 (VCAM-1), which is known to be upregulated during inflammation. In a mouse model of TBI utilizing central fluid percussion injury, free VCAM-1 antibody did not demonstrate superior targeting when comparing sham vs. TBI brain. However, the administration of VCAM-1-targeted nanocarriers (liposomes) exhibited a 10-fold higher targeting specificity in TBI brain than in sham control. Flow cytometry and confocal microscopy analysis confirmed that VCAM-1 liposomes were primarily taken up by brain endothelial cells post-TBI. Consequently, VCAM-1 liposomes represent a promising platform for the targeted delivery of therapeutics to the brain following traumatic brain injury.

MeSH terms

  • Animals
  • Blood-Brain Barrier* / drug effects
  • Blood-Brain Barrier* / metabolism
  • Brain Injuries, Traumatic* / drug therapy
  • Brain Injuries, Traumatic* / metabolism
  • Brain Injuries, Traumatic* / pathology
  • Disease Models, Animal
  • Drug Delivery Systems
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism
  • Liposomes
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Nanoparticles* / chemistry
  • Vascular Cell Adhesion Molecule-1* / metabolism

Substances

  • Vascular Cell Adhesion Molecule-1
  • Liposomes

Grants and funding

S.O. received funding from the American Heart Association (Grant 23PRE1014444). J.N. received funding from the American Heart Association (Grant 916172). B.J.K received funding from National Health Institute (K08-NS110929). O.A.M.-C. received funding from the American Heart Association (Grant 19CDA34590001). J.S.B. and V.M.R. received support from the Cardiovascular Institute of the University of Pennsylvania. V.M.R. received funding from National Institute of Health (R01 HL155106, R01 HL128398, R01 HL143806). J.S.B. received funding from National Institute of Health (K08-HL-138269, R01-HL-153510, R01-HL-160694, R01-HL-157189, R21-AI-166778-01). D.H.S received funding from the Paul G. Allen Family Foundation and National Institute of Health (U54 NS115322). AHA: https://www.heart.org/en/get-involved/ways-to-give?form=FUNPHPZDXBX&s_src=23L511AEMG&s_subsrc=fy23_jun_sem_google_text_&utm_medium=paid&utm_campaign=dr+fy23+june&utm_source=sem+google&utm_content=prospecting-remarketing+sem+general&utm_term=text&gad=1&gclid=CjwKCAjwp6CkBhB_EiwAlQVyxUMZ_FbtTs7VO9Lig6RdFLrTCBLy_fDCRjQoyJToLTNRKw3B3axoQhoC4ZwQAvD_BwE&gclsrc=aw.ds CVI: https://www.med.upenn.edu/cvi/funded-dream-teams.html NIH: https://www.nih.gov/grants-funding The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.