Anti-acetylcholinesterase and toxicity against Artemia salina of chitosan microparticles loaded with essential oils of Cymbopogon flexuosus, Pelargonium x ssp and Copaifera officinalis

Int J Biol Macromol. 2021 Jan 15:167:1361-1370. doi: 10.1016/j.ijbiomac.2020.11.090. Epub 2020 Nov 17.

Abstract

Essential oils (EOs) are bioactive compounds with therapeutic potential for use as alternatives or as support to conventional treatments. However, EOs present limitations, such as sensibility to environmental factors, which can be overcome through microencapsulation. The objective of this study was to produce, by spray drying, chitosan microparticles (CMs) loaded with EO of Lemongrass (Cymbopogon flexuosus), Geranium (Pelargonium x ssp) and Copaiba (Copaifera officinalis). Physicochemical and biological characterization of these microparticles showed that CMs presented spherical morphology, had an average size range of 2-3 μm with positive zeta potential (ZP) values, and enhanced thermal stability, compared to free EO. The encapsulation efficiency (EE) ranged from 4.8-58.6%, depending on the oil's properties. In vitro EO release from CMs was determined at different pHs, with 94% release observed in acid media. All microparticles were non-hemolytic at concentrations of up to 0.1 mg·mL-1. EOs and CMs presented acetylcholinesterase (AChE) inhibition activity (IC 50 ranged from 11.92 to 28.18 μg·mL-1). Geranium and Copaiba EOs presented higher toxicity against Artemia salina, and greater inhibition of acetylcholinesterase, indicating potential bioactivity for Alzheimer's disease (AD). Our findings demonstrate that CM systems may show promise for the controlled release of these EOs.

Keywords: Acetylcholinesterase; Chitosan microparticles; Copaiba oil; Geranium essential oil; Lemongrass essential oil.

MeSH terms

  • Animals
  • Artemia / drug effects*
  • Blood / drug effects
  • Capsules / chemistry*
  • Chitosan / chemistry*
  • Cholinesterase Inhibitors / pharmacology*
  • Cholinesterase Inhibitors / toxicity
  • Cymbopogon / chemistry*
  • Cymbopogon / toxicity
  • Fabaceae / chemistry*
  • Fabaceae / toxicity
  • Hemolysis
  • Hot Temperature
  • Humans
  • Hydrogen-Ion Concentration
  • Inhibitory Concentration 50
  • Microscopy, Electron, Scanning
  • Oils, Volatile / analysis*
  • Oils, Volatile / chemistry
  • Particle Size
  • Pelargonium / chemistry*
  • Pelargonium / toxicity
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Capsules
  • Cholinesterase Inhibitors
  • Oils, Volatile
  • Chitosan