Charge-converting nanocarriers: Phosphorylated polysaccharide coatings for overcoming intestinal barriers

Int J Biol Macromol. 2024 Nov;281(Pt 2):136308. doi: 10.1016/j.ijbiomac.2024.136308. Epub 2024 Oct 5.

Abstract

For the design of charge-converting nanocarriers (NCs), cationic lipid-based NCs containing curcumin as model drug were coated with phosphorylated starch (NC-SP) and phosphorylated dextran (NC-DP). NCs showed a drug encapsulation efficiency of 94 % and had a mean size of 175 to 180 nm. The recorded zeta potential of the core NC (cNC) was +8.3 mV, whereas it reversed to -10.6 mV and -7.4 mV after decorating with SP and DP, respectively. Furthermore, a 3-fold higher amount of curcumin having been incorporated in these NCs remained stable within 2 h of UV exposure indicating a photoprotective effect of this delivery system. Charge-converting properties were confirmed by cleavage with intestinal alkaline phosphatase (IAP) and resulted in a zeta potential shift of Δ15.4 mV for NC-SP and Δ11.2 mV for NC-DP. NC-SP and NC-DP showed enhanced mucus permeating properties compared to cNC, that were additionally confirmed by an up to 2.2-fold improved cellular uptake on mucus secreting Caco-2/HT29-MTX cells. According to these results, NC-SP and NC-DP coatings hold promise as a viable and efficient strategy for charge-converting NCs.

Keywords: Charge reversal; Nanoemulsions; Nanoparticles; Phosphatase; Polysaccharides; Zeta potential.

MeSH terms

  • Alkaline Phosphatase / metabolism
  • Caco-2 Cells
  • Curcumin* / chemistry
  • Curcumin* / pharmacology
  • Dextrans / chemistry
  • Drug Carriers* / chemistry
  • HT29 Cells
  • Humans
  • Intestinal Mucosa / drug effects
  • Intestinal Mucosa / metabolism
  • Nanoparticles / chemistry
  • Particle Size
  • Phosphorylation / drug effects
  • Polysaccharides / chemistry
  • Polysaccharides / pharmacology
  • Starch / chemistry

Substances

  • Drug Carriers
  • Curcumin
  • Polysaccharides
  • Alkaline Phosphatase
  • Dextrans
  • Starch