A novel approach to oral iron delivery using ferrous sulphate loaded solid lipid nanoparticles

Int J Pharm. 2013 Nov 18;456(2):400-7. doi: 10.1016/j.ijpharm.2013.08.070. Epub 2013 Sep 5.

Abstract

Iron (Fe) loaded solid lipid nanoparticles (SLN's) were formulated using stearic acid and iron absorption was evaluated in vitro using the cell line Caco-2 with intracellular ferritin formation as a marker of iron absorption. Iron loading was optimised at 1% Fe (w/w) lipid since an inverse relation was observed between initial iron concentration and SLN iron incorporation efficiency. Chitosan (Chi) was included to prepare chitosan coated SLN's. Particle size analysis revealed a sub-micron size range (300.3±31.75 nm to 495.1±80.42 nm), with chitosan containing particles having the largest dimensions. As expected, chitosan (0.1%, 0.2% and 0.4% w/v) conferred a net positive charge on the particle surface in a concentration dependent manner. For iron absorption experiments equal doses of Fe (20 μM) from selected formulations (SLN-FeA and SLN-Fe-ChiB) were added to Caco-2 cells and intracellular ferritin protein concentrations determined. Caco-2 iron absorption from SLN-FeA (583.98±40.83 ng/mg cell protein) and chitosan containing SLN-Fe-ChiB (642.77±29.37 ng/mg cell protein) were 13.42% and 24.9% greater than that from ferrous sulphate (FeSO4) reference (514.66±20.43 ng/mg cell protein) (p≤0.05). We demonstrate for the first time preparation, characterisation and superior iron absorption in vitro from SLN's, suggesting the potential of these formulations as a novel system for oral iron delivery.

Keywords: Caco-2; Chitosan; Ferritin; Ferrous sulfate; Iron supplementation; Solid lipid nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Caco-2 Cells
  • Cell Survival / drug effects
  • Cell Survival / physiology
  • Drug Delivery Systems / methods*
  • Ferrous Compounds / administration & dosage*
  • Ferrous Compounds / chemistry
  • Humans
  • Iron / administration & dosage*
  • Iron / chemistry
  • Lipids / administration & dosage*
  • Lipids / chemistry
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry

Substances

  • Ferrous Compounds
  • Lipids
  • ferrous sulfate
  • Iron