Nanofiber-based delivery of therapeutic peptides to the brain

Mariarosa Mazza, Rebecca Notman, Jamshed Anwar, Alison Rodger, Matthew Hicks, Gary Parkinson, Dave McCarthy, Tina Daviter, Julian Moger, Natalie Garrett, Tania Mead, Michael Briggs, Andreas G. Schätzlein, Ijeoma F. Uchegbu*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

67 Citations (Scopus)


The delivery of therapeutic peptides and proteins to the central nervous system is the biggest challenge when developing effective neuropharmaceuticals. The central issue is that the blood-brain barrier is impermeable to most molecules. Here we demonstrate the concept of employing an amphiphilic derivative of a peptide to deliver the peptide into the brain. The key to success is that the amphiphilic peptide should by design self-assemble into nanofibers wherein the active peptide epitope is tightly wrapped around the nanofiber core. The nanofiber form appears to protect the amphiphilic peptide from degradation while in the plasma, and the amphiphilic nature of the peptide promotes its transport across the blood-brain barrier. Therapeutic brain levels of the amphiphilic peptide are achieved with this strategy, compared with the absence of detectable peptide in the brain and the consequent lack of a therapeutic response when the underivatized peptide is administered.

Original languageEnglish
Pages (from-to)1016-1026
Number of pages11
JournalACS Nano
Issue number2
Publication statusPublished - 26 Feb 2013
Externally publishedYes


  • blood-brain barrier
  • dalargin
  • nanofibers
  • palmitoyl dalargin
  • peptide brain delivery
  • self-assembly


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