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基于木质素的球形结构及其在改善固态西拉普利稳定性中的应用。

Lignin-Based Spherical Structures and Their Use for Improvement of Cilazapril Stability in Solid State.

机构信息

Institute of Chemical Technology and Engineering, Faculty of Chemical Technology, Poznan University of Technology, Berdychowo 4, PL-60965 Poznan, Poland.

Chair and Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Grunwaldzka 6, PL-60780 Poznan, Poland.

出版信息

Molecules. 2020 Jul 9;25(14):3150. doi: 10.3390/molecules25143150.

Abstract

Biopolymer-based spherical particles exhibit unique properties including narrow sizes and many functional groups on their surfaces. Therefore, they show great potential for application in many scientific and industrial processes. The main aim of this study was to prepare lignin-based spherical particles with the use of a cationic surfactant, hexadecyl(trimethyl)ammonium bromide (CTAB). In the first step, different preparation procedures were tested with varying parameters, including biopolymer and surfactant ratios, lignin filtration, and experimental time. The morphological and dispersion characteristics of the materials were determined to select the best samples with the most promising properties, which could then be tested for their acute toxicity. It was observed that almost all materials were characterized by spherical shapes in micro- and nanosizes. The sample with the best physicochemical properties was used for further analysis and then tested for medical applications: the improvement of the stability of a drug molecule, cilazapril (CIL). The formulated material (CIL@LC-2a 1:1 wt./wt.) exhibited outstanding properties and significantly improved the stability of cilazapril as tested in conditions of increased temperature and humidity. Lignin spherical particles may be employed as a promising material for shielding other active compounds from decomposition.

摘要

基于生物聚合物的球形颗粒具有独特的性质,包括其表面的窄粒径和许多功能基团。因此,它们在许多科学和工业过程中具有巨大的应用潜力。本研究的主要目的是使用阳离子表面活性剂十六烷基三甲基溴化铵(CTAB)制备基于木质素的球形颗粒。在第一步中,测试了不同的制备程序,包括生物聚合物和表面活性剂的比例、木质素过滤和实验时间等参数。通过确定材料的形态和分散特性,选择了具有最有前途性质的最佳样品,然后对其进行急性毒性测试。结果表明,几乎所有材料的微观和纳米级都呈现出球形。具有最佳物理化学性质的样品被用于进一步分析,然后用于医学应用的测试:改善药物分子西拉普利(CIL)的稳定性。所制备的材料(CIL@LC-2a 1:1 wt./wt.)表现出优异的性质,显著提高了在高温高湿条件下西拉普利的稳定性。木质素球形颗粒可用作一种有前途的材料,用于保护其他活性化合物免受分解。

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