Effect of borneol as a penetration enhancer on brain targeting of nanoliposomes: facilitate direct delivery to neurons

Nanomedicine (Lond). 2018 Nov;13(21):2709-2727. doi: 10.2217/nnm-2018-0282. Epub 2018 Sep 20.

Abstract

Aim: This study is aimed to evaluate borneol as a penetration enhancer to improve brain target of nanoliposome.

Materials & methods: Effects of borneol on pharmacokinetics, targeting efficiency, brain subareas distribution and neuron-targeting level and pathway were studied by fluorescence spectrophotometry and immunofluorescence.

Results: Borneol did not influence physicochemical property of doxorubicin hydrochloride nanoliposome (Dox-nanoLips). Co-administration of Dox-nanoLips with borneol elevated brain-target efficiency due to selective distribution increase in the cerebral cortex and hippocampus without difference in contralateral hemisphere. Borneol improved neuronal-targeting level of Dox-nanoLips in the cortex, CA3 and dentate gyrus regions via opening tight junctions of blood-brain barrier and then bypassing astrocyte.

Conclusion: Borneol is potential to be a promising penetration enhancer for nanocarrier to target neurons.

Keywords: astrocyte; borneol; brain targeting; cerebral cortex; hippocampus; nanoliposomes; neurons; neurovascular units; penetration enhancer; vascular endothelial cell.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Astrocytes / drug effects
  • Blood-Brain Barrier / drug effects*
  • Camphanes / administration & dosage*
  • Camphanes / chemistry
  • Cerebral Cortex / drug effects
  • Doxorubicin / administration & dosage
  • Doxorubicin / chemistry
  • Humans
  • Liposomes / administration & dosage
  • Liposomes / chemistry
  • Mice
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Neurons / drug effects*

Substances

  • Camphanes
  • Liposomes
  • Doxorubicin
  • isoborneol