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采用负载硫酸亚铁的固体脂质纳米粒的新型口服铁传递方法。

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

机构信息

Department of Human & Health Sciences, University of Westminster, 115 New Cavendish Street, London W1W 6UW, United Kingdom.

出版信息

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.

摘要

铁(Fe)负载固体脂质纳米粒(SLN)是使用硬脂酸制备的,并通过 Caco-2 细胞系评估体外铁吸收,以细胞内铁蛋白形成作为铁吸收的标志物。铁负载优化为 1%(w/w)脂质,因为观察到初始铁浓度与 SLN 铁掺入效率之间存在反比关系。壳聚糖(Chi)被包括在内以制备壳聚糖包被的 SLN。粒径分析显示亚微米尺寸范围(300.3±31.75nm 至 495.1±80.42nm),壳聚糖含有的颗粒具有最大的尺寸。正如预期的那样,壳聚糖(0.1%,0.2%和 0.4%w/v)以浓度依赖的方式在颗粒表面赋予净正电荷。对于铁吸收实验,从选定制剂(SLN-FeA 和 SLN-Fe-ChiB)添加等量的 Fe(20μM)到 Caco-2 细胞中,并确定细胞内铁蛋白蛋白浓度。从 SLN-FeA(583.98±40.83ng/mg 细胞蛋白)和含壳聚糖的 SLN-Fe-ChiB(642.77±29.37ng/mg 细胞蛋白)吸收的 Caco-2 铁分别比硫酸亚铁(FeSO4)参考(514.66±20.43ng/mg 细胞蛋白)高 13.42%和 24.9%(p≤0.05)。我们首次证明了从 SLN 制备、表征和体外优越的铁吸收,这表明这些制剂作为口服铁传递的新型系统具有潜力。

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