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设计可食用纳米乳剂的界面以调节神经保护抗氧化剂的生物利用度。

Design of the interface of edible nanoemulsions to modulate the bioaccessibility of neuroprotective antioxidants.

机构信息

Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, University of Castilla-La Mancha, Albacete, Spain; Regional Centre of Biomedical Research (CRIB),University of Castilla-La Mancha, Albacete, Spain.

Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, University of Castilla-La Mancha, Albacete, Spain; Regional Centre of Biomedical Research (CRIB),University of Castilla-La Mancha, Albacete, Spain.

出版信息

Int J Pharm. 2015 Jul 25;490(1-2):209-18. doi: 10.1016/j.ijpharm.2015.05.031. Epub 2015 May 18.

DOI:10.1016/j.ijpharm.2015.05.031
PMID:25997659
Abstract

Most frequently the use of bioactive molecules for the supplementation of food and beverages is hampered by stability limitations or inadequate intestinal absorption. This work evaluates in vitro the role that the interface of the nanoemulsion has on the physicochemical properties, the stability behavior and the enzymatic degradation after oral intake. For that purpose three soybean oil (SB) formulations were studied. These formulations were based on the emulsifier lecithin but modified with two non-ionic surfactants Pluronic(®) F68 (PF68) or Pluronic(®) F127 (PF127) yielding (i) SB-NE (only lecithin on the interface), (ii) SB-NE PF68 (lecithin plus PF68) and 9 (iii) SB-NE PF127 (lecithin plus PF127). All the formulations tested were low polydispersed and showed a size of about 200 nm and ζ-potential of -50 mV. The in vitro colloidal stability assay showed that lecithin itself was able to promote that formulations reach unaltered to the small intestine and facilitate the absorption of the antioxidant payload on a tunable fashion there (with in vitro bioaccessibility values from around 40% up to a 70%). PF68 was able to sterically stabilize the formulation against the aggregation induced by the pH and electrolytes of the simulated gastrointestinal track; however, this surfactant was easily displaced by the lipases of the simulated intestinal milieu being unable to modulate the digestion pattern of the oil droplets in the small intestine. Finally, PF127 displayed a strong steric potential that dramatically reduced the interaction of the oil droplets with lipases in vitro, which will compromise the capacity of the formulation to improve the bioaccessibility of the loaded antioxidant.

摘要

大多数情况下,生物活性分子在食品和饮料中的应用受到稳定性限制或肠道吸收不足的阻碍。本工作评估了纳米乳液界面在理化性质、口服摄入后的稳定性行为和酶降解方面的作用。为此,研究了三种大豆油 (SB) 配方。这些配方基于乳化剂卵磷脂,但用两种非离子表面活性剂 Pluronic(®) F68 (PF68) 或 Pluronic(®) F127 (PF127) 进行修饰,得到 (i) SB-NE(界面仅含卵磷脂)、(ii) SB-NE PF68(卵磷脂加 PF68)和 9 (iii) SB-NE PF127(卵磷脂加 PF127)。所有测试的配方均为低多分散性,粒径约为 200nm,ζ-电位为-50mV。体外胶体稳定性试验表明,卵磷脂本身能够促进配方到达小肠而不发生变化,并以可调节的方式促进抗氧化剂有效载荷的吸收(体外生物利用度值在 40%左右到 70%)。PF68 能够通过模拟胃肠道的 pH 值和电解质来对抗聚集,从而稳定配方;然而,这种表面活性剂很容易被模拟肠环境中的脂肪酶取代,无法调节油滴在小肠中的消化模式。最后,PF127 表现出很强的空间位阻,极大地减少了油滴与体外脂肪酶的相互作用,这将影响配方提高负载抗氧化剂生物利用度的能力。

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