Nose-to-brain peptide delivery - The potential of nanotechnology

Bioorg Med Chem. 2018 Jun 1;26(10):2888-2905. doi: 10.1016/j.bmc.2017.11.001. Epub 2017 Nov 4.

Abstract

Nose-to-brain (N-to-B) delivery offers to protein and peptide drugs the possibility to reach the brain in a non-invasive way. This article is a comprehensive review of the state-of-the-art of this emerging peptide delivery route, as well as of the challenges associated to it. Emphasis is given on the potential of nanosized drug delivery carriers to enhance the direct N-to-B transport of protein or peptide drugs. In particular, polymer- and lipid- based nanocarriers are comparatively analyzed in terms of the influence of their physicochemical characteristics and composition on their in vivo fate and efficacy. The use of biorecognitive ligands and permeation enhancers in order to enhance their brain targeting efficiency is also discussed. The article concludes highlighting the early stage of this research field and its still unveiled potential. The final message is that more explicatory PK/PD studies are required in order to achieve the translation from preclinical to the clinical development phase.

Keywords: Intranasal drug administration; Lipid-based nanocarriers; Nanomedicine; Nanoparticles; Nose-to-brain delivery; Olfactory; Polymer-based nanocarriers; Protein drugs; Therapeutic peptides.

Publication types

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

MeSH terms

  • Administration, Intranasal
  • Animals
  • Brain / metabolism*
  • Drug Carriers / chemistry
  • Drug Carriers / metabolism*
  • Drug Delivery Systems / methods
  • Humans
  • Nanoparticles / chemistry
  • Nanoparticles / metabolism*
  • Nanotechnology / methods
  • Nasal Mucosa / metabolism
  • Peptides / administration & dosage*
  • Peptides / pharmacokinetics
  • Proteins / administration & dosage*
  • Proteins / pharmacokinetics

Substances

  • Drug Carriers
  • Peptides
  • Proteins