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天然腐殖酸盐荧光光谱中的二阶散射猝灭作为形成稳定超分子体系以递送难溶性抗病毒药物的示踪剂——以芒果苷和法匹拉韦为例

Second-Order Scattering Quenching in Fluorescence Spectra of Natural Humates as a Tracer of Formation Stable Supramolecular System for the Delivery of Poorly Soluble Antiviral Drugs on the Example of Mangiferin and Favipiravir.

作者信息

Morozova Mariya A, Tumasov Vladimir N, Kazimova Ilaha V, Maksimova Tatiana V, Uspenskaya Elena V, Syroeshkin Anton V

机构信息

Department of Pharmaceutical and Toxicological Chemistry, Medical Institute, Peoples' Friendship University of Russia (RUDN University), 6 Miklukho-Maklaya Street, 117198 Moscow, Russia.

出版信息

Pharmaceutics. 2022 Mar 31;14(4):767. doi: 10.3390/pharmaceutics14040767.

Abstract

In the present work, the methods of dynamic light scattering and fluorescence spectroscopy were applied to study the optical properties of aqueous dilutions of the humic substances complex (HC) as a potential drug delivery system. The supramolecular structures in the humate solution were characterized as monodisperse systems of the submicron range with a tendency to decrease in particle size with a decrease in the dry matter concentration. The slightly alkaline medium (8.3) of the studied aqueous dilutions of HC causes the absence of a pronounced fluorescence maximum in the region from 400 to 500 nm. However, the presence of an analytically significant, inversely proportional to the concentration second-order scattering (SOS) signal at 2λ = λ was shown. In the examples of the antiviral substances mangiferin and favipiravir, it was shown that the use of the humic complex as a drug carrier makes it possible to increase the solubility by several times and simultaneously obtain a system with a smaller particle size of the dispersed phase. It has been shown that HC can interact with mangiferin and favipiravir to form stable structures, which lead to a significant decrease in SOS intensities on HC SOS spectra. The scattering wavelengths, λ/λ, were registered at 350 nm/750 nm for mangiferin and 365 nm/730 nm for favipiravir, respectively. The increments of the scattering intensities (I0/I) turned out to be proportional to the concentration of antiviral components in a certain range of concentrations.

摘要

在本研究中,应用动态光散射和荧光光谱法研究了腐殖质复合物(HC)水稀释液作为潜在药物递送系统的光学性质。腐殖酸盐溶液中的超分子结构被表征为亚微米范围的单分散体系,且随着干物质浓度的降低,粒径有减小的趋势。所研究的HC水稀释液的微碱性介质(8.3)导致在400至500nm区域内没有明显的荧光最大值。然而,在2λ = λ处显示出存在与浓度成反比的、具有分析意义的二级散射(SOS)信号。以抗病毒物质芒果苷和法匹拉韦为例,结果表明,使用腐殖质复合物作为药物载体能够使溶解度提高数倍,同时获得分散相粒径更小的体系。研究表明,HC可与芒果苷和法匹拉韦相互作用形成稳定结构,这导致HC SOS光谱上的SOS强度显著降低。芒果苷的散射波长λ/λ分别在350nm/750nm处记录,法匹拉韦的散射波长λ/λ分别在365nm/730nm处记录。在一定浓度范围内,散射强度的增量(I0/I)与抗病毒成分的浓度成正比。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/16cb/9030643/967eea69fdae/pharmaceutics-14-00767-g001.jpg

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