Fabrication, physicochemical characterization and In vitro anticancer activity of nerolidol encapsulated solid lipid nanoparticles in human colorectal cell line

Colloids Surf B Biointerfaces. 2022 Jul:215:112520. doi: 10.1016/j.colsurfb.2022.112520. Epub 2022 Apr 26.

Abstract

Nerolidol is a sesquiterpene that occurs naturally and possesses a diverse set of biological characteristics including anticancer activity but has limited solubility, bioavailability, and fast hepatic metabolism. The goal of this study was to develop a nanocarrier system encapsulating a bioactive as well as to evaluate its efficacy in Human Colorectal Cell Line. Solid lipid nanoparticles were fabricated by the emulsion solvent evaporation method and determined the particle size, polydispersity index (PDI), zeta potential, % entrapment efficiency, scanning electron microscopy (SEM), transmission electron microscopy (TEM), drug-excipient interaction study of developed nanoparticles. MTT assay was used to assess the cytotoxicity of formulations in vitro. Nerolidol loaded solid lipid nanoparticles (NR-LNPs) have presented satisfactory properties: mean particles diameter of 159 ± 4.89 nm, PDI of 0.32 ± 0.01, the zeta potential value was found to be -10 ± 1.97 and % entrapment efficiency 71.3% ± 6.11. The formulations demonstrated enhanced biological activity due to enhanced solubility and stability of the bioactive after loading into a nanoformulation along with the better internalization inside the cells.

Keywords: Anti-cancer activity; Apoptosis; Caco-2 cells; Nerolidol; Solid lipid nanoparticles.

MeSH terms

  • Cell Line
  • Colorectal Neoplasms* / drug therapy
  • Drug Carriers / chemistry
  • Humans
  • Lipids / chemistry
  • Liposomes
  • Nanoparticles* / chemistry
  • Particle Size
  • Sesquiterpenes* / pharmacology

Substances

  • Drug Carriers
  • Lipid Nanoparticles
  • Lipids
  • Liposomes
  • Sesquiterpenes
  • nerolidol