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

M Gulrez Zariwala, Naba Elsaid, Timothy L Jackson, Francisco Corral López, Sebastien Farnaud, Satyanarayana Somavarapu, Derek Renshaw

Research output: Contribution to journalArticle

20 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)400-7
Number of pages8
JournalScientia Pharmaceutica
Volume456
Issue number2
DOIs
Publication statusPublished - 18 Nov 2013

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ferrous sulfate
Nanoparticles
Iron
Lipids
Chitosan
Ferritins
Proteins

Keywords

  • Administration, Oral
  • Caco-2 Cells
  • Cell Survival
  • Drug Delivery Systems
  • Ferrous Compounds
  • Humans
  • Iron
  • Lipids
  • Nanoparticles
  • Journal Article
  • Research Support, Non-U.S. Gov't
  • Solid lipid nanoparticles
  • Ferrous-sulfate
  • Iron-supplementation
  • Chitosan
  • Caco-2
  • Ferritin

Cite this

A novel approach to oral iron delivery using ferrous sulphate loaded solid lipid nanoparticles. / Zariwala, M Gulrez; Elsaid, Naba; Jackson, Timothy L; Corral López, Francisco; Farnaud, Sebastien; Somavarapu, Satyanarayana; Renshaw, Derek.

In: Scientia Pharmaceutica, Vol. 456, No. 2, 18.11.2013, p. 400-7.

Research output: Contribution to journalArticle

Zariwala, M Gulrez ; Elsaid, Naba ; Jackson, Timothy L ; Corral López, Francisco ; Farnaud, Sebastien ; Somavarapu, Satyanarayana ; Renshaw, Derek. / A novel approach to oral iron delivery using ferrous sulphate loaded solid lipid nanoparticles. In: Scientia Pharmaceutica. 2013 ; Vol. 456, No. 2. pp. 400-7.
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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.",
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AU - Zariwala, M Gulrez

AU - Elsaid, Naba

AU - Jackson, Timothy L

AU - Corral López, Francisco

AU - Farnaud, Sebastien

AU - Somavarapu, Satyanarayana

AU - Renshaw, Derek

N1 - Copyright © 2013 Elsevier B.V. All rights reserved.

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Y1 - 2013/11/18

N2 - 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.

AB - 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.

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KW - Cell Survival

KW - Drug Delivery Systems

KW - Ferrous Compounds

KW - Humans

KW - Iron

KW - Lipids

KW - Nanoparticles

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

KW - Solid lipid nanoparticles

KW - Ferrous-sulfate

KW - Iron-supplementation

KW - Chitosan

KW - Caco-2

KW - Ferritin

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DO - 10.1016/j.ijpharm.2013.08.070

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VL - 456

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EP - 407

JO - Scientia Pharmaceutica

JF - Scientia Pharmaceutica

SN - 0036-8709

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ER -