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The effect of surface charge on oral absorption of polymeric nanoparticles
Biomaterials Science ( IF 6.6 ) Pub Date : 2018-01-22 00:00:00 , DOI: 10.1039/c7bm01096f
Xiao-Jiao Du 1, 2, 3, 4, 5 , Ji-Long Wang 4, 6, 7, 8 , Shoaib Iqbal 4, 6, 7, 8 , Hong-Jun Li 1, 2, 3, 4, 5 , Zhi-Ting Cao 4, 6, 7, 8 , Yu-Cai Wang 4, 6, 7, 8 , Jin-Zhi Du 1, 2, 3, 4, 5 , Jun Wang 1, 2, 3, 4, 5
Affiliation  

Surface charge plays an important role in determining the interactions of nanoparticles with biological components. Substantial studies have demonstrated that surface charge affects the fate of nanoparticles after intravenous administration; however, few studies have investigated the effect of surface charge on the bioavailability and absorption of nanoparticles after oral administration. In this study, polymeric nanoparticles with a similar particle size and surface polyethylene glycol (PEG) density, but with varying surface charges (positive, negative and neutral), were developed to study the effect of surface charge on the oral absorption of polymeric nanoparticles. The nanoparticles were constructed from polyethylene glycol-block-polylactic acid (PEG-PLA) with the incorporation of lipid components with different charges. Our results suggested that the positive surface charge facilitated the cellular uptake and transport of nanoparticles through both Caco-2 cells in vitro and small intestinal epithelial cells in vivo. The positively charged nanoparticles showed a favorable distribution in the small intestine, and significantly improved the oral bioavailability. This study presents valuable information towards the design of nanoparticles for improved oral drug delivery.

中文翻译:

表面电荷对聚合物纳米颗粒口服吸收的影响

表面电荷在确定纳米颗粒与生物组分的相互作用中起重要作用。大量研究表明,静脉内给药后表面电荷会影响纳米颗粒的命运。然而,很少有研究研究口服后表面电荷对纳米颗粒生物利用度和吸收的影响。在这项研究中,开发了具有相似粒径和表面聚乙二醇(PEG)密度但具有不同表面电荷(正电荷,负电荷和中性电荷)的聚合物纳米颗粒,以研究表面电荷对聚合物纳米颗粒口服吸收的影响。纳米粒子由聚乙二醇嵌段构建-聚乳酸(PEG-PLA),并带有不同电荷的脂质成分。我们的结果表明,表面正电荷通过两个Caco-2细胞促进了细胞摄取和纳米颗粒的运输体外和小肠上皮细胞在体内。带正电的纳米颗粒在小肠中显示出有利的分布,并显着提高了口服生物利用度。这项研究为纳米颗粒的设计提供了有价值的信息,以改善口服药物的递送。
更新日期:2018-01-22
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