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将多孔淀粉与聚氧乙烯氢化蓖麻油RH40相结合以提高双去甲氧基姜黄素的溶解度、稳定性和生物利用度。

Combining porous starch and polyoxyethylene hydrogenated castor oil RH40 to enhance the solubility, stability, and bioavailability of bisdemethoxycurcumin.

作者信息

Liang Xuewei, Duan Xuehui, Du Yan, Tang Zhongjie, Ma Zhongyi, Zhu Ning, Yang Andong, Tang Yixuan

机构信息

School of Pharmaceutical Sciences & Institute of Materia Medica, Medical Science and Technology Innovation Center, Key Laboratory for Biotechnology Drugs of National Health Commission, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, Shandong 250117, China; Medical Research Institute, College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.

School of Pharmaceutical Sciences & Institute of Materia Medica, Medical Science and Technology Innovation Center, Key Laboratory for Biotechnology Drugs of National Health Commission, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, Shandong 250117, China.

出版信息

Int J Biol Macromol. 2025 May;309(Pt 4):143189. doi: 10.1016/j.ijbiomac.2025.143189. Epub 2025 Apr 15.

DOI:10.1016/j.ijbiomac.2025.143189
PMID:40246090
Abstract

Bisdemethoxycurcumin (BDC) is an important ingredient derived from the food spice turmeric. Although BDC exhibits various pharmacological effects, it is characterized by poor water solubility and limited stability under light. Considering that the high specific surface area of porous starch (PS) renders it an ideal carrier for the encapsulation of active compounds, and polyoxyethylene‑hydrogenated castor oil RH40 (RH40) is an effective solubilizer for BDC, the current study optimized the PS/RH40/BDC formulation to combine these advantages. Consequently, a PS/RH40/BDC ratio of 10:3:1 was identified as optimal (RH-PS/BDC). Characterization using scanning electron microscopy, X-ray diffractometry, Fourier-transform infrared spectroscopy, Brunauer-Emmett-Teller analysis, and stability testing indicated that BDC was amorphously encapsulated within the RH-PS system, thereby leading to enhanced stability and solubility. Furthermore, cellular uptake experiments revealed a significant increase of RH-PS/BDC. In terms of the enhancement mechanism, RH40 can reduce cell membrane fluidity and open tight junctions between intestinal epithelial cells, thereby facilitating BDC absorption. In vivo pharmacodynamic analysis confirmed that RH-PS/BDC effectively inhibited LPS-induced cerebral neuritis. Overall, this study demonstrates the role of PS in combination with RH40 in enhancing the stability and bioavailability of BDC. This simple and efficient preparation strategy is promising for future research and product development.

摘要

双去甲氧基姜黄素(BDC)是一种源自食品香料姜黄的重要成分。尽管BDC具有多种药理作用,但其特点是水溶性差且在光照下稳定性有限。鉴于多孔淀粉(PS)的高比表面积使其成为封装活性化合物的理想载体,且聚氧乙烯氢化蓖麻油RH40(RH40)是BDC的有效增溶剂,本研究优化了PS/RH40/BDC配方以结合这些优点。因此,确定PS/RH40/BDC的比例为10:3:1是最佳的(RH-PS/BDC)。通过扫描电子显微镜、X射线衍射、傅里叶变换红外光谱、布鲁诺尔-埃米特-泰勒分析和稳定性测试进行的表征表明,BDC以无定形形式封装在RH-PS系统中,从而提高了稳定性和溶解度。此外,细胞摄取实验显示RH-PS/BDC显著增加。就增强机制而言,RH40可降低细胞膜流动性并打开肠上皮细胞之间的紧密连接,从而促进BDC的吸收。体内药效学分析证实,RH-PS/BDC有效抑制脂多糖诱导的脑神经炎。总体而言,本研究证明了PS与RH40结合在提高BDC稳定性和生物利用度方面的作用。这种简单有效的制备策略对未来的研究和产品开发具有前景。

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