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基于两亲性透明质酸衍生物的新型自缔合多相纳米结构软载体

Novel self-associative and multiphasic nanostructured soft carriers based on amphiphilic hyaluronic acid derivatives.

作者信息

Eenschooten Corinne, Vaccaro Andrea, Delie Florence, Guillaumie Fanny, Tømmeraas Kristoffer, Kontogeorgis Georgios M, Schwach-Abdellaoui Khadija, Borkovec Michal, Gurny Robert

机构信息

Novozymes Biopharma DK A/S, Krogshoejvej 36, DK-2880 Bagsværd, Denmark; Technical University of Denmark, Department of Chemical and Biochemical Engineering, Centre for Energy Resources Engineering (CERE), Building 229, DK-2800 Lyngby, Denmark.

University of Geneva, Department of Inorganic, Analytical and Applied Chemistry, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland.

出版信息

Carbohydr Polym. 2012 Jan 4;87(1):444-451. doi: 10.1016/j.carbpol.2011.08.004. Epub 2011 Aug 10.

Abstract

The purpose of the present study was to investigate the physicochemical properties in aqueous media of amphiphilic hyaluronic acid (HA) derivatives obtained by reaction of HA's hydroxyl groups with octenyl succinic anhydride (OSA). The self-associative properties of the resulting octenyl succinic anhydride-modified hyaluronic acid (OSA-HA) derivatives were studied by fluorescence spectroscopy using Nile Red as fluorophore. The morphology, size and surface charge of the OSA-HA assemblies were determined by transmission electron microscopy, dynamic light scattering and by measuring their electrophoretic mobility, respectively. OSA-HA was shown to spontaneously self-associate in aqueous media into negatively charged spherical and multiphasic nanostructures with a hydrodynamic diameter between 170 and 230nm and to solubilize hydrophobic compounds such as Nile Red. This was a good indication that OSA-HA could be used as building block for the formulation of soft nanocarriers towards the encapsulation and controlled delivery of hydrophobic active ingredients or drugs.

摘要

本研究的目的是研究通过透明质酸(HA)的羟基与辛烯基琥珀酸酐(OSA)反应得到的两亲性透明质酸衍生物在水性介质中的物理化学性质。使用尼罗红作为荧光团,通过荧光光谱法研究了所得辛烯基琥珀酸酐修饰的透明质酸(OSA-HA)衍生物的自缔合性质。分别通过透射电子显微镜、动态光散射以及测量其电泳迁移率来确定OSA-HA聚集体的形态、尺寸和表面电荷。结果表明,OSA-HA在水性介质中能自发自缔合形成带负电荷的球形和多相纳米结构,其流体动力学直径在170至230nm之间,并且能够溶解尼罗红等疏水性化合物。这充分表明OSA-HA可作为构建软纳米载体的基础材料,用于包封和控制递送疏水性活性成分或药物。

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