基因斯坦与氨基酸的同形系统:对增强溶解度和生物活动的研究
Ewa Garbiec1, Natalia Rosiak1, Przemysław Zalewski1
1Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, 3 Rokietnicka St., 60-806 Poznan, Poland.
Pharmaceutics
|December 23, 2023
概括
杰尼斯泰因 (Genistein) 是一种植物性物质.
科学领域:
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
- 材料科学 材料科学 材料科学
背景情况:
- 基因斯坦是一种异黄,表现出抗氧化和抗糖尿病的特性,但由于溶解性差而受到限制.
- 低溶解度阻碍了基尼斯坦的生物可用性和治疗疗效.
- 开发提高基因斯坦溶解度的策略对于其制药应用至关重要.
研究的目的:
- 使用共形系统增强基因斯坦的可溶性和生物活性.
- 研究通过计算方法选择的氨基酸在形成基因斯坦共形系统中的潜力.
- 评估开发的基因斯坦共形系统的物理化学性质,稳定性和生物性能.
主要方法:
- 合成了与氨酸和氨酸一起生成的基因斯坦的共同形态系统.
- 无形状态通过X射线粉末衍射 (XRPD) 证实.
- 使用热重力测量 (TGA),微分扫描热量测量 (DSC),里埃变换红外光谱 (FTIR) 和扫描电子显微镜 (SEM) 的表征.
- 在6个月内评估身体稳定性.
- 在水性介质中确定表面溶解度.
- 在实验室中,使用并行人工膜透性试验 (PAMPA) 评估胃肠道透性.
- 通过DPPH和CUPRAC试验评估的抗氧化活性.
- 测量了α-葡萄糖酶抑制.
- 玻璃过渡温度 (Tg) 通过 DSC.确定.
主要成果:
- 与氨酸和氨酸共同无形系统成功合成,并确认是无形的.
- 含素的系统显示出明显溶解度和抗氧化活性最显著的改善.
- 与阿卡尔相比,这两种共同形态系统都表现出增强的α-葡萄糖酶抑制.
- 在6个月的储存期内,系统保持了物理稳定性.
- DSC和FTIR分析证实了系统的同质性和分子相互作用.
结论:
- 结合氨酸和氨酸的共同形态系统有效地提高了基因斯坦的可溶性和生物特性.
- 基于素的系统在提高溶解度和抗氧化活性方面表现出卓越的性能.
- 这些共同形态系统具有显著的潜力,可以提高基因斯坦的治疗效果,特别是在2型糖尿病管理方面.
- 这些系统的进一步开发可以改善药物输送和患者的治疗结果.
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