Single-stranded β-1,3-1,6-glucan as a carrier for improved dissolution and membrane permeation of poorly water-soluble compounds

Carbohydr Polym. 2020 Nov 1:247:116698. doi: 10.1016/j.carbpol.2020.116698. Epub 2020 Jun 29.

Abstract

The ability of a water-soluble, single-stranded β-1,3/1,6-glucan (ssβ-glucan), recovered by hydrothermal treatment, to enhance the solubility and membrane permeability of poorly water-soluble compounds was examined. As a poorly water-soluble model compound, quercetin (QUE) was used. The aqueous solubility of spray-dried particles (SDPs) of QUE/ssβ-glucan was significantly enhanced compared with that of the untreated QUE powder and the physical mixture of QUE/ssβ-glucan. Fourier-transform infrared spectra and small-angle X-ray scattering suggested strong interactions between ssβ-glucan and QUE in the SDPs, which was attributable to QUE entrapment in the helical ssβ-glucan structure. The amount of QUE infused into Caco-2 cells from QUE/ssβ-glucan SDPs was 16-fold and 5-fold higher than the amount infused from untreated QUE powder and the physical mixture of QUE/ssβ-glucan, respectively. These results showed that water-soluble ssβ-glucan improved QUE dissolution and membrane permeability.

Keywords: Permeability enhancement; Quercetin; Solubility enhancement; β-1,3/1,6-Glucan.

MeSH terms

  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Caco-2 Cells
  • Cell Membrane Permeability*
  • Cell Survival / drug effects
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Humans
  • Microscopy, Electron, Scanning
  • Powder Diffraction
  • Powders / analysis
  • Powders / chemistry
  • Quercetin / chemistry
  • Quercetin / pharmacology
  • Scattering, Small Angle
  • Solubility*
  • Spectroscopy, Fourier Transform Infrared
  • Spray Drying
  • Water / chemistry
  • X-Ray Diffraction
  • beta-Glucans / chemistry*

Substances

  • Antioxidants
  • Drug Carriers
  • Powders
  • beta-Glucans
  • Water
  • beta-1,6-glucan
  • beta-1,3-glucan
  • Quercetin