Chitosan-alginate nanoparticles as effective oral carriers to improve the stability, bioavailability, and cytotoxicity of curcumin diethyl disuccinate

Carbohydr Polym. 2021 Mar 15:256:117426. doi: 10.1016/j.carbpol.2020.117426. Epub 2020 Nov 24.

Abstract

Curcumin diethyl disuccinate (CDD) is an ester prodrug of curcumin that has better chemical stability in phosphate buffer (pH 7.4) and anticancer activities against MDA-MB-231 human breast cancer cells and Caco-2 cells than curcumin. However, a major drawback of CDD is its poor water solubility and low bioavailability in the gastrointestinal tract. To overcome these problems, a nanoformulation was developed using chitosan/alginate nanoparticles (CANPs) under the optimal condition as previously derived by statistical optimization. The CDD-loaded CANPs (CDD-CANPs) were found to exhibit good stability after exposure to simulated digestive fluids and ultraviolet light, and a sustained-release profile of CDD in the simulated digestive and body fluids. The in vitro release pattern fitted well to the Peppas-Sahlin model, indicating that the release of CDD was mainly governed by diffusion. Compared to free CDD, the CDD-CANPs showed better stability, bioaccessibility, bioavailability, cellular uptake, and cytotoxicity against HepG2 cells.

Keywords: Bioaccessibility; Bioavailability; Chitosan-alginate nanoparticles; Curcumin diethyl disuccinate.

MeSH terms

  • Alginates / chemistry*
  • Biological Availability
  • Cell Line, Tumor
  • Chitosan / chemistry*
  • Curcumin / analogs & derivatives*
  • Curcumin / chemistry
  • Drug Carriers*
  • Hep G2 Cells
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Nanoparticles / chemistry*
  • Nanotechnology / methods
  • Particle Size
  • Prodrugs
  • Solubility
  • Succinates / chemistry*
  • Ultraviolet Rays

Substances

  • Alginates
  • Drug Carriers
  • Prodrugs
  • Succinates
  • curcumin diethyl disuccinate
  • Chitosan
  • Curcumin