Enhanced therapeutic benefit of quercetin-loaded phytosome nanoparticles in ovariectomized rats

Chem Biol Interact. 2017 Jun 1:271:30-38. doi: 10.1016/j.cbi.2017.04.026. Epub 2017 Apr 29.

Abstract

Quercetin, a dietary flavonol phytoestrogen, has many health benefits but it is poorly absorbed when administered orally. To improve its bioavailability, we prepared quercetin-loaded phytosome nanoparticles (QP) using the thin film hydration method. The prepared nano-formulations were characterized using different techniques. Transmission electron microscopy revealed the homogeneously spherical, well and uniformly dispersed, nano-sized nature of QP. Dynamic light scattering measurements of QP (70 ± 7.44 nm) also confirmed this. Stability of the formed nanoparticles was established via zeta potential determination. The prepared QP exhibited very high encapsulation efficiency (98.4%). The estrogenic activity of QP, concerning inflammation, oxidative stress, bone, lipid profile, blood glucose level and weight gain, was investigated in ovariectomized rat model using 10 and 50 mg/kg/day oral doses for 4 weeks. Treatment with QP showed significant increase in serum calcium, inorganic phosphorus and glutathione content. Whereas, it significantly decreased serum alkaline phosphatase, acid phosphatase, malondialdehyde level, tumor necrosis factor-alpha and glucose level and improved lipid profile. Consequently, the results obtained confirm the superiority of QP over free quercetin at the same doses as a promising hormone replacement therapy.

Keywords: Nanoparticles; Ovariectomized rats; Phytoestrogen; Phytosome; Quercetin.

MeSH terms

  • Animals
  • Biological Availability
  • Blood Glucose / drug effects
  • Body Weight / drug effects
  • Drug Stability
  • Female
  • Microscopy, Electron, Transmission
  • Nanoparticles* / ultrastructure
  • Ovariectomy
  • Oxidative Stress / drug effects
  • Particle Size
  • Quercetin / pharmacology*
  • Rats
  • Tumor Necrosis Factor-alpha / drug effects
  • Tumor Necrosis Factor-alpha / metabolism*

Substances

  • Blood Glucose
  • Tumor Necrosis Factor-alpha
  • Quercetin