title: Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: preparation, characterisation and in vitro evaluation.
abstract: The objective of this study was to encapsulate iron in nanocarriers formulated with ascorbyl palmitate and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine polyethylene glycol (DSPE-PEG) for oral delivery. Blank and iron (Fe) loaded nanocarriers were prepared by a modified thin film method using ascorbyl palmitate and DSPE-PEG. Surface charge of the nanocarriers was modified by the inclusion of chitosan (CHI) during the formulation process. Blank and iron loaded ascorbyl palmitate/DSPE nanocarriers were visualised by transmission electron microscopy (TEM) and physiochemical characterisations of the nanocarriers carried out to determine the mean particle size and zeta potential. Inclusion of chitosan imparted a net positive charge on the nanocarrier surface and also led to an increase in mean particle size. Iron entrapment in ascorbyl palmitate-Fe and ascorbyl palmitate-CHI-Fe nanocarriers was 67% and 76% respectively, suggesting a beneficial effect of chitosan on nanocarrier Fe entrapment. Iron absorption was estimated by measuring Caco-2 cell ferritin formation using ferrous sulphate as a reference standard. Iron absorption from ascorbyl palmitate-Fe (592.17±21.12 ng/mg cell protein) and ascorbyl palmitate-CHI-Fe (800.12±47.6 ng/mg, cell protein) nanocarriers was 1.35-fold and 1.5-fold higher than that from free ferrous sulphate, respectively (505.74±23.73 ng/mg cell protein) (n=6, p<0.05). This study demonstrates for the first time preparation and characterisation of iron loaded ascorbyl palmitate/DSPE PEG nanocarriers, and that engineering of the nanocarriers with chitosan leads to a significant augmentation of iron absorption.
authors: Faculty of Science & Technology, University of Westminster, 115 New Cavendish Street, London W1W 6UW, United Kingdom. Electronic address: m.zariwala@westminster.ac.uk.
authors: M Gulrez
authors: MG
authors: Zariwala
authors: Department of Life Sciences, University of Bedfordshire, Luton, Bedfordshire LU1 3JU, United Kingdom.
authors: Sebastien
authors: S
authors: Farnaud
authors: Department of Pharmaceutics, UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
authors: Zahra
authors: Z
authors: Merchant
authors: Department of Pharmaceutics, UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
authors: Satyanarayana
authors: S
authors: Somavarapu
authors: Faculty of Science & Technology, University of Westminster, 115 New Cavendish Street, London W1W 6UW, United Kingdom.
authors: Derek
authors: D
authors: Renshaw
mesh_terms: D000042:Absorption / Q000187:drug effects; D000284:Administration, Oral; D001205:Ascorbic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D018938:Caco-2 Cells; D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D007501:Iron / Q000008:administration & dosage / Q000494:pharmacology*; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D055672:Static Electricity
chemical_list: D004337:Drug Carriers; D010714:Phosphatidylethanolamines; C038089:1,2-distearoylphosphatidylethanolamine; D011092:Polyethylene Glycols; D007501:Iron; D001205:Ascorbic Acid; C031226:6-O-palmitoylascorbic acid
keywords: Ascorbyl palmitate; Caco-2; Chitosan; Ferrous sulphate; Fortification; Nanocarriers