Chitosan nanoparticle-mediated nose-to-brain delivery of naringenin: Attenuating memory decline in experimental animals via behavioural assessment and modulation of biochemical parameters

Int J Biol Macromol. 2025 Jan:286:138336. doi: 10.1016/j.ijbiomac.2024.138336. Epub 2024 Dec 10.

Abstract

Naringenin, a flavonoid with potent antioxidant properties, faces low bioavailability, limiting its clinical application in Alzheimer's disease. This study developed naringenin-loaded chitosan nanoparticles (NAR-CNPs) for nose-to-brain delivery using the ionic gelation method. The NAR-CNPs exhibited an average particle size of 112.35 ± 1.55 nm, zeta potential of 15.36 ± 2.05 mV, and entrapment efficiency of 69.49 ± 1.88 %, with a sustained release profile (65.80 % over 8 h). Ex vivo permeation studies showed a 1.91-fold higher steady-state flux for NAR-CNPs compared to naringenin suspension, indicating enhanced brain penetration. The NAR-CNPs were safe for goat nasal mucosa and improved cognitive function in scopolamine-induced demented mice, whereas significantly reducing acetylcholinesterase activity (p < 0.001) and increasing antioxidant enzyme activities in the brain of experimental mice. Concurrently, the level of malondialdehyde was decreased in the brain, indicating reduced lipid peroxidation. Histopathological analysis showed a significant increase in neuronal count in NAR-CNPs treated animals compared to control group. These findings suggest that intranasally administered NAR-CNPs hold promise for treating cognitive impairment, though further studies are needed for clinical translation.

Keywords: Behavioural alterations and changes in biochemical parameters; Intranasal application; Naringenin-loaded chitosan nanoparticle.

MeSH terms

  • Acetylcholinesterase / metabolism
  • Administration, Intranasal*
  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / pharmacology
  • Behavior, Animal / drug effects
  • Brain* / drug effects
  • Brain* / metabolism
  • Brain* / pathology
  • Chitosan* / chemistry
  • Chitosan* / pharmacology
  • Drug Carriers / chemistry
  • Flavanones* / administration & dosage
  • Flavanones* / chemistry
  • Flavanones* / pharmacology
  • Goats
  • Lipid Peroxidation / drug effects
  • Male
  • Memory Disorders / drug therapy
  • Mice
  • Nanoparticles* / chemistry
  • Nasal Mucosa / drug effects
  • Nasal Mucosa / metabolism
  • Particle Size

Substances

  • Chitosan
  • naringenin
  • Flavanones
  • Drug Carriers
  • Antioxidants
  • Acetylcholinesterase