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用于提高姜黄素生物利用度的纳米乳剂及其安全性评价:乳化剂类型的影响

Nanoemulsions for Enhancement of Curcumin Bioavailability and Their Safety Evaluation: Effect of Emulsifier Type.

作者信息

Gonçalves Raquel F S, Martins Joana T, Abrunhosa Luís, Vicente António A, Pinheiro Ana C

机构信息

Centre of Biological Engineering, University of Minho, 4715-057 Braga, Portugal.

出版信息

Nanomaterials (Basel). 2021 Mar 23;11(3):815. doi: 10.3390/nano11030815.

Abstract

This work aimed at evaluating the effects of different emulsifiers on curcumin-loaded nanoemulsions' behavior during digestion, its safety and absorption, to develop nanoemulsions that provide safety and improved curcumin functionality. Nanoemulsions (NEs) were produced using two bio-based (lecithin (LEC) and rhamnolipids (RHAM)) and one synthetic (Tween80 (TWE)) emulsifier at similar concentrations. Different NEs were subjected to in vitro digestion. The cytotoxicity and permeability tests were performed in Caco-2 cells. NE_TWE were stable during all phases of in vitro digestion, whereas NE_LEC and NE_RHAM were found to be unstable from the gastric phase. NE_TWE showed 100% of free fatty acids released, followed by NE_RHAM and NE_LEC. Curcumin's bioaccessibility and stability increased in the following order: NE_LEC > NE_RHAM > NE_TWE. NE_LEC and NE_TWE did not show cytotoxic effects in any of the concentrations tested, while NE_RHAM presented high cytotoxicity in all concentrations tested. The apparent permeability coefficients were determined for NE_LEC and NE_TWE; however, the results were not statistically different. These results showed that the emulsifier used has a high impact on nanoemulsions' behavior under the digestion process and on their cytotoxicity. This work contributed to the state-of-the-art's progress on the development of safer curcumin delivery systems with improved functionality, particularly regarding the proper selection of ingredients to produce said systems.

摘要

本研究旨在评估不同乳化剂对载姜黄素纳米乳剂在消化过程中的行为、安全性和吸收的影响,以开发出具有安全性且能改善姜黄素功能的纳米乳剂。使用两种生物基乳化剂(卵磷脂(LEC)和鼠李糖脂(RHAM))以及一种合成乳化剂(吐温80(TWE))以相似浓度制备纳米乳剂。对不同的纳米乳剂进行体外消化实验。在Caco-2细胞中进行细胞毒性和渗透性测试。NE_TWE在体外消化的所有阶段均保持稳定,而NE_LEC和NE_RHAM从胃消化阶段就被发现不稳定。NE_TWE释放的游离脂肪酸达100%,其次是NE_RHAM和NE_LEC。姜黄素的生物可及性和稳定性按以下顺序增加:NE_LEC > NE_RHAM > NE_TWE。NE_LEC和NE_TWE在任何测试浓度下均未显示细胞毒性作用,而NE_RHAM在所有测试浓度下均表现出高细胞毒性。测定了NE_LEC和NE_TWE的表观渗透系数;然而,结果在统计学上没有差异。这些结果表明,所用乳化剂对纳米乳剂在消化过程中的行为及其细胞毒性有很大影响。这项工作推动了在开发具有更优功能的更安全姜黄素递送系统方面的前沿进展,特别是在生产所述系统时对成分的合理选择方面。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3c63/8004751/2354f207316e/nanomaterials-11-00815-g001.jpg

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