Development of novel therapeutics targeting the blood–brain barrier: from barrier to carrier

Jia Li, Meng Zheng, Olga Shimoni, William A. Banks , Ashley I. Bush, Jennifer R. Gamble, Bingyang Shi*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

55 Citations (Scopus)
55 Downloads (Pure)


The blood–brain barrier (BBB) is a highly specialized neurovascular unit, initially described as an intact barrier to prevent toxins, pathogens, and potentially harmful substances from entering the brain. An intact BBB is also critical for the maintenance of normal neuronal function. In cerebral vascular diseases and neurological disorders, the BBB can be disrupted, contributing to disease progression. While restoration of BBB integrity serves as a robust biomarker of better clinical outcomes, the restrictive nature of the intact BBB presents a major hurdle for delivery of therapeutics into the brain. Recent studies show that the BBB is actively engaged in crosstalk between neuronal and the circulatory systems, which defines another important role of the BBB: as an interfacing conduit that mediates communication between two sides of the BBB. This role has been subject to extensive investigation for brain-targeted drug delivery and shows promising results. The dual roles of the BBB make it a unique target for drug development. Here, recent developments and novel strategies to target the BBB for therapeutic purposes are reviewed, from both barrier and carrier perspectives.
Original languageEnglish
Article number2101090
Pages (from-to)1-27
Number of pages27
JournalAdvanced Science
Issue number16
Early online date3 Jun 2021
Publication statusPublished - 18 Aug 2021

Bibliographical note

Copyright the Author(s) 2021. Version archived for private and non-commercial use with the permission of the author/s and according to publisher conditions. For further rights please contact the publisher.


  • blood–brain barrier
  • brain diseases
  • drug delivery
  • nanomedicine
  • nanotechnology


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