In situ nanostructured hydrogel of resveratrol for brain targeting: in vitro-in vivo characterization

Drug Deliv Transl Res. 2018 Oct;8(5):1460-1470. doi: 10.1007/s13346-018-0540-6.

Abstract

The purpose of conducting the present research work was to develop resveratrol nanostructured in situ gel for the treatment of Alzheimer's disease. Resveratrol loaded lipid carrier was prepared by melt emulsification-probe sonication method, and the final product was evaluated for particle size (132 ± 11.90 nm), polydispersity index (0.209 ± 0.005), zeta potential (- 23 ± 3.79 mV), drug loading (9.26 ± 3.79%), and entrapment efficiency (74 ± 11.40%). Following incorporation of the resveratrol nanostructured lipid carrier in gellan gum and xanthan gum, in situ gel was formulated and characterized. The optimized in situ gel showed fivefold higher permeation across the nasal mucosa as compared to resveratrol suspension-based in situ gel. Finally, optimized in situ gel was evaluated using in vivo pharmacodynamic study by the scopolamine-induced amnesia model in rats using Morris Water Maze test. It showed significant improvement in memory function in rats treated with optimized in situ gel as compared to orally administered resveratrol suspension. The enhanced permeation across nasal mucosa and improved memory function suggest that the resveratrol nanostructured lipid carrier-based in situ gel could be an effective and promising approach for the treatment of Alzheimer's disease.

Keywords: Gellan gum; In situ gel; Nanostructured lipid carrier; Nasal route; Resveratrol.

Publication types

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

MeSH terms

  • Administration, Intranasal
  • Administration, Oral
  • Alzheimer Disease / drug therapy
  • Amnesia / chemically induced
  • Amnesia / drug therapy*
  • Animals
  • Disease Models, Animal
  • Drug Carriers / chemistry
  • Emulsions
  • Hydrogels / chemistry*
  • In Vitro Techniques
  • Male
  • Nanostructures / chemistry*
  • Particle Size
  • Polysaccharides, Bacterial / chemistry
  • Rats
  • Resveratrol / administration & dosage*
  • Resveratrol / chemistry
  • Resveratrol / pharmacokinetics*
  • Scopolamine / adverse effects*

Substances

  • Drug Carriers
  • Emulsions
  • Hydrogels
  • Polysaccharides, Bacterial
  • gellan gum
  • Scopolamine
  • Resveratrol
  • xanthan gum