Evaluation of intranasal delivery route of drug administration for brain targeting

Brain Res Bull. 2018 Oct:143:155-170. doi: 10.1016/j.brainresbull.2018.10.009. Epub 2018 Oct 25.

Abstract

The acute or chronic drug treatments for different neurodegenerative and psychiatric disorders are challenging from several aspects. The low bioavailability and limited brain exposure of oral drugs, the rapid metabolism, elimination, the unwanted side effects and also the high dose to be added mean both inconvenience for the patients and high costs for the patients, their family and the society. The reason of low brain penetration of the compounds is that they have to overcome the blood-brain barrier which protects the brain against xenobiotics. Intranasal drug administration is one of the promising options to bypass blood-brain barrier, to reduce the systemic adverse effects of the drugs and to lower the doses to be administered. Furthermore, the drugs administered using nasal route have usually higher bioavailability, less side effects and result in higher brain exposure at similar dosage than the oral drugs. In this review the focus is on giving an overview on the anatomical and cellular structure of nasal cavity and absorption surface. It presents some possibilities to enhance the drug penetration through the nasal barrier and summarizes some in vitro, ex vivo and in vivo technologies to test the drug delivery across the nasal epithelium into the brain. Finally, the authors give a critical evaluation of the nasal route of administration showing its main advantages and limitations of this delivery route for CNS drug targeting.

Keywords: CNS indication; Delivery enhancer techniques; Drug delivery; Intranasal administration; Transporter interactions.

Publication types

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

MeSH terms

  • Administration, Intranasal / methods*
  • Animals
  • Blood-Brain Barrier / drug effects
  • Brain / metabolism
  • Drug Administration Routes
  • Drug Delivery Systems / methods
  • Humans
  • Models, Animal
  • Nasal Cavity / anatomy & histology
  • Nasal Cavity / drug effects*
  • Trigeminal Nerve / drug effects