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亲水性金纳米粒子与地塞米松药物的直接相互作用:负载和释放研究。

Direct interaction of hydrophilic gold nanoparticles with dexamethasone drug: loading and release study.

机构信息

Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.

Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy; Center for Nanotechnology for Engineering (CNIS), Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.

出版信息

J Colloid Interface Sci. 2014 Mar 15;418:52-60. doi: 10.1016/j.jcis.2013.11.063. Epub 2013 Dec 4.

Abstract

Water-soluble gold nanoparticles functionalized by sodium 3-mercapto-1-propansulfonate (Au-3MPS) were synthesized with different Au/thiol molar ratios for their ability to interact with biomolecules. In particular, a synthetic glucocorticoid steroid, i.e. dexamethasone (DXM) was selected. Herein, the formation of the Au-3MPS/DXM bioconjugate is reported. Au-3MPS nanoparticles show a plasmon resonance at 520 nm, have a spherical morphology and average size of 7-10 nm. The total number of gold atoms was estimated to be about 10600, with a surface component of 8800 atoms and a number of thiol ligands of about 720, roughly one anchored thiol every 10 surface gold atoms. The drug-nanoparticle interaction occurs through the fluorine atom of DXM and Au(I) atoms on the gold nanoparticle surface. The 3MPS ligands closely pack apart each other to leave room for the DXM, that lies at the gold surface in an unusual, almost parallel feature. The loading efficiency of DXM on Au-3MPS was assessed in the range 70-80%, depending on the thiol content. Moreover, our studies confirmed the drug release of about 70% in 5 days. Thanks to their unique properties, i.e. high water solubility, small size and almost monodispersity, Au-3MPS display high potential in biotechnological and biomedical applications, mainly for the loading and release of water insoluble drugs.

摘要

采用不同的 Au/硫醇摩尔比合成了 3-巯基-1-丙磺酸(Au-3MPS)功能化的水溶性金纳米粒子,以研究其与生物分子相互作用的能力。特别是选择了一种合成的糖皮质激素类固醇,即地塞米松(DXM)。本文报道了 Au-3MPS/DXM 生物缀合物的形成。Au-3MPS 纳米粒子在 520nm 处表现出等离子体共振,具有球形形态和 7-10nm 的平均尺寸。估计金原子的总数约为 10600 个,表面成分有 8800 个原子,硫醇配体的数量约为 720 个,大约每 10 个表面金原子就有一个锚定的硫醇。药物-纳米粒子相互作用通过 DXM 的氟原子和金纳米粒子表面上的 Au(I)原子发生。3MPS 配体彼此紧密排列,为 DXM 留出空间,DXM 以不寻常的、几乎平行的方式位于金表面。Au-3MPS 对 DXM 的负载效率在 70-80%范围内,这取决于硫醇的含量。此外,我们的研究证实,在 5 天内约有 70%的药物释放。由于其独特的性质,如高水溶性、小尺寸和几乎单分散性,Au-3MPS 在生物技术和生物医学应用中具有很高的潜力,主要用于负载和释放水不溶性药物。

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