Central nervous system delivery of molecules across the blood-brain barrier

Neurochem Int. 2021 Mar;144:104952. doi: 10.1016/j.neuint.2020.104952. Epub 2021 Jan 2.


Therapies targeting neurological conditions such as Alzheimer's or Parkinson's diseases are hampered by the presence of the blood-brain barrier (BBB). During the last decades, several approaches have been developed to overcome the BBB, such as the use of nanoparticles (NPs) based on biomaterials, or alternative methods to open the BBB. In this review, we briefly highlight these strategies and the most recent advances in this field. Limitations and advantages of each approach are discussed. Combination of several methods such as functionalized NPs targeting the receptor-mediated transcytosis system with the use of magnetic resonance imaging-guided focused ultrasound (FUS) might be a promising strategy to develop theranostic tools as well as to safely deliver therapeutic molecules, such as drugs, neurotrophic factors or antibodies within the brain parenchyma.

Keywords: Blood-brain barrier; Brain diseases; Central nervous system drug delivery; Cyclodextrins; Nanoparticles; PLGA.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Blood-Brain Barrier / drug effects*
  • Blood-Brain Barrier / metabolism
  • Brain / drug effects*
  • Brain / metabolism
  • Brain / pathology
  • Central Nervous System / drug effects
  • Central Nervous System / metabolism
  • Central Nervous System / pathology
  • Central Nervous System Diseases / drug therapy*
  • Central Nervous System Diseases / metabolism
  • Central Nervous System Diseases / pathology
  • Drug Delivery Systems / methods*
  • Humans
  • Nanoparticles / administration & dosage*
  • Nanoparticles / metabolism