Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System

Molecules. 2021 Dec 11;26(24):7497. doi: 10.3390/molecules26247497.

Abstract

Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its in vitro dissolution and hepatoprotective effects, resulting in increased oral bioavailability. Using the aqueous phase titration approach and the creation of pseudo-ternary phase diagrams with Capryol-PGMC (oil phase), Tween-80 (surfactant), and Transcutol-HP (co-emulsifier), various SNEDDS of LUT were generated. SNEDDS were assessed for droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), and percent of transmittance (percent T) after undergoing several thermodynamic stability and self-nanoemulsification experiments. When compared to LUT suspension, the developed SNEDDS revealed considerable LUT release from all SNEDDS. Droplet size was 40 nm, PDI was <0.3, ZP was -30.58 mV, RI was 1.40, percent T was >98 percent, and drug release profile was >96 percent in optimized SNEDDS of LUT. For in vivo hepatoprotective testing in rats, optimized SNEDDS was chosen. When compared to LUT suspension, hepatoprotective tests showed that optimized LUT SNEDDS had a substantial hepatoprotective impact. The findings of this investigation suggested that SNEDDS could improve bioflavonoid LUT dissolution rate and therapeutic efficacy.

Keywords: SNEDDS; bioflavonoid; droplet size; hepatoprotective effects; luteolin.

MeSH terms

  • Administration, Oral
  • Animals
  • Carbon Tetrachloride / pharmacology
  • Drug Delivery Systems*
  • Emulsions / administration & dosage
  • Emulsions / metabolism
  • Emulsions / pharmacology
  • Liver / drug effects*
  • Liver / metabolism
  • Luteolin / administration & dosage
  • Luteolin / metabolism
  • Luteolin / pharmacology*
  • Male
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Particle Size
  • Protective Agents / administration & dosage
  • Protective Agents / metabolism
  • Protective Agents / pharmacology*
  • Rats
  • Rats, Wistar
  • Solubility
  • Thermodynamics

Substances

  • Emulsions
  • Protective Agents
  • Carbon Tetrachloride
  • Luteolin