Hesperetin-loaded polymeric nanofibers: assessment of bioavailability and neuroprotective effect

Drug Dev Ind Pharm. 2023 Feb;49(2):240-247. doi: 10.1080/03639045.2023.2201625. Epub 2023 Apr 19.

Abstract

Objective: The purpose of the study is to assess the bioavailability and neuroprotective effect of hesperetin (Hesp)-loaded nanofibers.

Methods: Electrospinning was used to create and characterize polyvinyl pyrrolidone-based Hesp-loaded nanofibers. To evaluate the produced nanofibers, preclinical studies were conducted. The study involved five groups of Wistar rats, and the treatments were administered as follows. Group 1 (control) was given regular saline for 14 d. On the 14th day, Group 2 was given scopolamine. Group 3 was given donepezil for 14 d and then scopolamine on the 14th. Group 4 was given Hesp for 14 d and then scopolamine on the 14th. Group 5 was given Hesp-loaded nanofibers for 14 d, followed by scopolamine on the 14th. On the 14th day, rats' memory was tested using Cook's pole climbing apparatus and the Morris water maze (MWM). On the 15th day, rats from each group were slaughtered, brain tissues were separated, and biochemical and histological analyses were performed. In addition, in vitro dissolution experiments and pharmacokinetic studies were carried out.

Results: When compared to the control group, scopolamine-treated rats had considerably longer escape latency times, as well as increased acetylcholinesterase (AChE) activity, lipid peroxidation, degeneration, and inflammation in the hippocampus. These parameters were greatly recovered by donepezil and Hesp-loaded nanofibers that had been pretreated. Because of the greatly improved bioavailability of Hesp, the Hesp-loaded nanofibers significantly protected rats from scopolamine-induced amnesia.

Conclusions: Hesp-loaded nanofibers have an excellent neuroprotective effect against scopolamine-induced amnesia due to enhanced bioavailability.

Keywords: Hesperetin; amnesia; bioavailability; dissolution; nanofibers; neuroprotection.

MeSH terms

  • Acetylcholinesterase / metabolism
  • Acetylcholinesterase / pharmacology
  • Acetylcholinesterase / therapeutic use
  • Amnesia / chemically induced
  • Amnesia / drug therapy
  • Animals
  • Biological Availability
  • Donepezil / pharmacology
  • Maze Learning
  • Nanofibers*
  • Neuroprotective Agents* / pharmacology
  • Rats
  • Rats, Wistar
  • Scopolamine / adverse effects

Substances

  • Donepezil
  • Neuroprotective Agents
  • hesperetin
  • Acetylcholinesterase
  • Scopolamine