Nose to brain drug delivery - A promising strategy for active components from herbal medicine for treating cerebral ischemia reperfusion

Pharmacol Res. 2020 Sep;159:104795. doi: 10.1016/j.phrs.2020.104795. Epub 2020 Apr 8.


Cerebral ischemia reperfusion injury (CIRI), one of the major causes of death from stroke in the world, not only causes tremendous damage to human health, but also brings heavy economic burden to society. Current available treatments for CIRI, including mechanical therapies and drug therapies, are often accompanied by significant side-effects. Therefore, it is necessary to discovery new strategies for treating CIRI. Many studies have confirmed that the herbal medicine has the advantages of abundant resources, good curative effect and little side effects, which can be used as potential drug for treatment of CIRI through multiple targets. It's known that oral administration commonly has low bioavailability, and injection administration is inconvenient and unsafe. Many drugs can't delivery to brain through routine pathways due to the blood-brain-barrier (BBB). Interestingly, increasing evidences have suggested the nasal administration is a potential direct route to transport drug into brain avoiding the BBB and has the characteristics of high bioavailability for treating brain diseases. Therefore, intranasal administration can be treated as an alternative way to treat brain diseases. In the present review, effective methods to treat CIRI by using active ingredients derived from herbal medicine through nose to brain drug delivery (NBDD) are updated and discussed, and some related pharmacological mechanisms have also been emphasized. Our present study would be beneficial for the further drug development of natural agents from herbal medicines via NBDD.

Keywords: Active components; Apigenin (PubChem CID: 5280443); Artemisinin (PubChem CID: 452191); Baicalin (PubChem CID: 64982); Berberine (PubChem CID: 2353); Bilobalide (PubChem CID: 73581); Breviscapine (PubChem CID: 6426802); Calycosin (PubChem CID: 5280448); Cerebral ischemia reperfusion injury; Cimicifugoside H-1 (PubChem CID: 15241163); Curcumin (PubChem CID: 969516); Ferulic acid (PubChem CID: 445858); Formononetin (PubChem CID: 5280378); Gastrodin (PubChem CID: 115067); Geniposide (PubChem CID: 107848); Ginkgolide B (PubChem CID: 65243); Herbal medicine; Hydroxysafflor yellow A (PubChem CID: 6443665); Hyperoside (PubChem CID: 5281643); Intranasal administration; Isoliquiritigenin (PubChem CID: 638278); Ligustilide (PubChem CID: 5319022); Ligustrazine (PubChem CID:14296); Mangiferin (PubChem CID: 5281647); Matrine (PubChem CID: 91466); Morroniside (PubChem CID: 11304302); Nose to brain drug delivery; Osthole (PubChem CID: 10228); Paeoniflorin (PubChem CID: 442534); Picroside II (PubChem CID: 9849283); Proanthocyanidin (PubChem CID: 108065); Puerarin (PubChem CID: 5281807); Quercetin (PubChem CID: 5280343); Resveratrol (PubChem CID: 445154); Rutin (PubChem CID: 5280805); Salidroside (PubChem CID: 159278); Salvianolic acid B (PubChem CID: 11629084); Sinomenine (PubChem CID: 5459308); Tanshinone II (PubChem CID: 164676); Vitexin (PubChem CID: 5280441); α-Asarone (PubChem CID: 636822); β-Asarone (PubChem CID: 5281758).

Publication types

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

MeSH terms

  • Administration, Intranasal
  • Animals
  • Biological Availability
  • Brain / drug effects*
  • Brain / metabolism
  • Brain / pathology
  • Brain Ischemia / drug therapy*
  • Brain Ischemia / metabolism
  • Brain Ischemia / pathology
  • Drug Compounding
  • Humans
  • Nasal Mucosa / metabolism*
  • Plant Preparations / administration & dosage*
  • Plant Preparations / metabolism
  • Reperfusion Injury / drug therapy*
  • Reperfusion Injury / metabolism
  • Reperfusion Injury / pathology
  • Tissue Distribution


  • Plant Preparations