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机械化学方法,以获得多组分的菲塞输送系统,提高其溶解性和生物活性

Natalia Rosiak¹, Ewa Tykarska², Judyta Cielecka-Piontek¹

¹Department of Pharmacognosy and Biomaterials, Faculty of Pharmacy, Poznan University of Medical Sciences, 3 Rokietnicka St., 60-806 Poznan, Poland.

International journal of molecular sciences

|April 13, 2024

概括

这项研究使用机械化学开发了无溶剂的无形固体分散和含有素 (FIS). 最好的配方显著提高了FIS的溶解性,抗氧化剂和神经保护性质.

科学领域:

材料科学材料科学材料科学
制药科学制药科学
生物化学生物化学

背景情况:

菲塞 (FIS) 是一种具有抗氧化和神经保护潜力的天然黄类化合物.
较差的水溶性和生物可用性限制了FIS的治疗应用.
无形固体分散 (ASD) 和包含 (ASI) 可以提高药物的溶解性和疗效.

研究的目的:

为了准备无溶剂的二进制ASDs和三进制ASIs的fisetin (FIS).
调查无形化对FIS溶解度及其抗氧化和神经保护作用的影响.
为了确定最优的配方,以增强fisetin的交付.

主要方法:

机械化学制备ASDs (fisetin-Eudragit®) 和ASI (fisetin-Eudragit®-HP-β-cyclodextrin) 的机械化学制备.
使用X射线粉末衍射 (XRPD),差分扫描热度计 (DSC) 和里埃变换红外光谱法 (FT-IR) 的表征.
在体外评估表面溶解性,抗氧化能力 (ABTS,DPPH,CUPRAC,FRAP测定) 和神经保护 (AChE,BChE抑制测定). 还进行了分子对接.

主要成果:

证实了FIS在ASD和ASI中的无形性和完全混合性.
FT-IR分析揭示了稳定FIS无形状态的相互作用.
最佳配方,ASI_30_EPO,显示出126.5μg∙mL−1的表面溶解度.
ASI_30_EPO表现出强大的抗氧化剂 (例如,ABTS IC50 = 10.25 μg∙mL-1) 和神经保护作用 (AChE: 39.91%,BChE: 42.62%的抑制).

结论:

无溶剂的机械化学制剂有效地产生无形固体分散和纳入素.
形态化显著提高了菲塞的表面溶解性,抗氧化和神经保护性质.
开发的ASI配方有望改善菲塞的治疗潜力.

关键词:

无形固体分散的无形固体分散无形固体的包含性包括.素是素中的一种成分.改善了生物活动.混杂性混杂性混杂性分子对接的分子对接.溶解度溶解度溶解度溶解度

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