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岩藻依聚糖和壳聚糖静电包覆的纳米脂质体可增强芦丁的物理化学稳定性和生物利用度。

Fucoidan and chitosan electrostatically coated nanoliposomes enhance physicochemical stability and bioavailability of rutin.

作者信息

Han Jieyu, Pang Yuehong, Shen Xiaofang

机构信息

School of Food Science and Technology, Jiangnan University, Wuxi 214122, PR China.

School of Food Science and Technology, Jiangnan University, Wuxi 214122, PR China.

出版信息

Int J Biol Macromol. 2025 Apr;301:140450. doi: 10.1016/j.ijbiomac.2025.140450. Epub 2025 Jan 28.

DOI:10.1016/j.ijbiomac.2025.140450
PMID:39884615
Abstract

Rutin, a promising bioactive hydrophobic compound, suffers from poor physicochemical stability, resulting in low bioavailability. Herein, we used positively charged chitosan and negatively charged fucoidan as biopolymers coating rutin-nanoliposome (RNL) via electrostatic layer-by-layer self-assembly approach to prepare fucoidan/chitosan-coated rutin-nanoliposome (FC-RNL). The FC-RNL exhibited the encapsulation efficiency of 77.01% for rutin, with the particle size of 346 nm and a zeta potential of -33.5 mV under the optimized conditions (lecithin to rutin ratio of 10, 0.05 wt% fucoidan and 0.20 wt% chitosan). The results of Fourier transform infrared, X-ray diffraction, and transmission electron microscopy suggested that fucoidan/chitosan-coated nanoliposome could effectively load rutin. The coating of fucoidan and chitosan not only improved the retention rate of rutin (> 85 %) under thermal, oxidative and UV-light conditions, but also showed excellent stability over a wide pH range (pH 3.0-11.0) and high ionic strength (400 mM NaCl). In addition, FC-RNL was more stable than C-RNL and RNL at 4 °C for 5-week storage. In vitro simulated digestion indicated that FC-RNL significantly controlled the rutin release, and preserved 6.86 % and 50.47 % of rutin at the end of simulated gastric and intestinal digestion, respectively. Furthermore, FC-RNL exhibited satisfactory biocompatibility, and cellular uptake studies demonstrated that FC-RNL displayed the highest Rh123 uptake efficiency reaching approximately 189 %. This study provides an effective fucoidan/chitosan-coated nanoliposome carrier for the delivery of hydrophobic bioactive compounds within the functional food industry.

摘要

芦丁是一种很有前景的生物活性疏水化合物,但因其物理化学稳定性差,导致生物利用度低。在此,我们通过静电层层自组装方法,使用带正电荷的壳聚糖和带负电荷的岩藻依聚糖作为生物聚合物包裹芦丁纳米脂质体(RNL),制备了岩藻依聚糖/壳聚糖包裹的芦丁纳米脂质体(FC-RNL)。在优化条件下(卵磷脂与芦丁的比例为10、岩藻依聚糖为0.05 wt%、壳聚糖为0.20 wt%),FC-RNL对芦丁的包封率为77.01%,粒径为346 nm,ζ电位为 -33.5 mV。傅里叶变换红外光谱、X射线衍射和透射电子显微镜结果表明,岩藻依聚糖/壳聚糖包裹的纳米脂质体能够有效地负载芦丁。岩藻依聚糖和壳聚糖的包裹不仅提高了芦丁在热、氧化和紫外光条件下的保留率(> 85%),而且在较宽的pH范围(pH 3.0 - 11.0)和高离子强度(400 mM NaCl)下也表现出优异的稳定性。此外,在4℃储存5周时,FC-RNL比C-RNL和RNL更稳定。体外模拟消化表明,FC-RNL能显著控制芦丁的释放,在模拟胃和肠道消化结束时分别保留了6.86%和50.47%的芦丁。此外,FC-RNL表现出令人满意的生物相容性,细胞摄取研究表明,FC-RNL表现出最高的罗丹明123摄取效率,达到约189%。本研究为功能性食品工业中疏水性生物活性化合物的递送提供了一种有效的岩藻依聚糖/壳聚糖包裹的纳米脂质体载体。

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