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通过溶剂蒸发法将姜黄素负载于多孔淀粉中所增强的姜黄素的溶出度和生物利用度。

The dissolution and bioavailability of curcumin reinforced by loading into porous starch under solvent evaporation.

作者信息

Niu Ben, Li Zhiyu, Luan Cuirong, Zhao Beibei

机构信息

School of Food Science and Technology, Jiangnan University, Wuxi 214122, Jiangsu Province, People's Republic of China.

Fuzhou Institute of Oceanography, Minjiang University, Fuzhou 350108, Fujian Province, People's Republic of China; Department of Geography and Oceanography, Minjiang University, Fuzhou 350108, Fujian Province, People's Republic of China.

出版信息

Int J Biol Macromol. 2025 Jan;287:138611. doi: 10.1016/j.ijbiomac.2024.138611. Epub 2024 Dec 9.

DOI:10.1016/j.ijbiomac.2024.138611
PMID:39662552
Abstract

Curcumin is a polyphenol with anti-inflammatory and antitumorigenic properties. However, its low water solubility and bioavailability limit its use. In this study, porous starch supplemented with a solvent evaporation process was demonstrated as a highly loaded vehicle for curcumin (17.82 %) that could be efficiently solubilized over sustained periods. The migration of curcumin and its adsorption onto the surface of porous starch during solvent evaporation indicated that curcumin was deposited as amorphous globules in pores and encapsulated on the starch surface. The process was demonstrated to involve hydrogen bonding and hydrophobic interactions using infrared spectroscopy and particle dissociation experiments. Notably, the saturated solubility of curcumin in CU/PS in ionized water, ethanol, and acetic acid was 17.81×, 31.65×, and 26.53× greater than that of raw curcumin, respectively. In particular, it could slowly dissolve in simulated intestinal fluids and exhibited a higher cumulative dissociation (about 6 times that of raw curcumin). In vitro experiments using a colon adenocarcinoma cell line confirmed that curcumin loaded with porous starch enhanced cellular uptake and reduced IC of raw curcumin by 55 times. Thus, porous starch with a simple and efficient process provides new ideas for the design of drug delivery systems and is expected to inspire further development in reducing dosing intervals and maximizing therapeutic efficacy.

摘要

姜黄素是一种具有抗炎和抗肿瘤特性的多酚。然而,其低水溶性和生物利用度限制了它的应用。在本研究中,采用溶剂蒸发法制备的多孔淀粉被证明是一种高载药量的姜黄素载体(载药量为17.82%),能够在较长时间内有效地溶解姜黄素。溶剂蒸发过程中姜黄素的迁移及其在多孔淀粉表面的吸附表明,姜黄素以无定形小球的形式沉积在孔中,并包裹在淀粉表面。通过红外光谱和颗粒解离实验证明该过程涉及氢键和疏水相互作用。值得注意的是,姜黄素在离子水、乙醇和乙酸中的CU/PS饱和溶解度分别比姜黄素原料药高17.81倍、31.65倍和26.53倍。特别是,它能在模拟肠液中缓慢溶解,并表现出更高的累积解离度(约为姜黄素原料药的6倍)。使用结肠腺癌细胞系的体外实验证实,负载多孔淀粉的姜黄素增强了细胞摄取,并且将姜黄素原料药的半数抑制浓度降低了55倍。因此,具有简单高效工艺的多孔淀粉为药物递送系统的设计提供了新思路,有望在减少给药间隔和最大化治疗效果方面引发进一步的发展。

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