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通过天然生物聚合物实现基于脂质的递药系统的生物和热力学稳定化;控制释放和分子动力学模拟。

Biological and thermodynamic stabilization of lipid-based delivery systems through natural biopolymers; controlled release and molecular dynamics simulations.

机构信息

Department of Food Hygiene and Aquaculture, Faculty of Veterinary Medicine, Ferdowsi University of Mashhad, Mashhad, Iran.

Australasian Nanoscience and Nanotechnology Initiative (ANNI), Clayton, Victoria, Australia.

出版信息

Crit Rev Food Sci Nutr. 2024;64(22):7728-7747. doi: 10.1080/10408398.2023.2191281. Epub 2023 Mar 23.

Abstract

Nowadays, the use of lipid-based nanocarriers for the targeted and controlled delivery of a variety of hydrophobic and hydrophilic bioactive-compounds and drugs has increased significantly. However, challenges such as thermodynamic instability, oxidation, and degradation of lipid membranes, as well as the unintended release of loaded compounds, have limited the use of these systems in the food and pharmaceutical industries. Therefore, the present study reviews the latest achievements in evaluating the characteristics, production methods, challenges, functional, and biological stabilization strategies of lipid-based carriers (including changes in formulation composition, structural modification, membrane-rigidity, and finally monolayer or multilayer coating with biopolymers) in different conditions, as well as molecular dynamics simulations. The scientists' findings indicate the effect of natural biopolymers (such as chitosan, calcium alginate, pectin, dextran, xanthan, caseins, gelatin, whey-proteins, zein, and etc.) in modifying the external structure of lipid-based carriers, improving thermodynamic stability and resistance of membranes to physicochemical and mechanical tensions. However, depending on the type of bioactive compound as well as the design and production goals of the delivery-system, selecting the appropriate biopolymer has a significant impact on the stability of vesicles and maintaining the bioaccessibility of the loaded-compounds due to the stresses caused by the storage-conditions, formulation, processing and gastrointestinal tract.

摘要

如今,基于脂质的纳米载体被广泛应用于靶向和控制传递各种疏水性和亲水性生物活性化合物和药物。然而,脂质膜的热力学不稳定性、氧化和降解,以及载药化合物的意外释放等问题,限制了这些系统在食品和制药行业中的应用。因此,本研究综述了评价脂质载体特性、生产方法、挑战、功能和生物稳定性策略的最新进展,包括改变配方组成、结构修饰、膜刚性,以及最终用生物聚合物进行单层或多层包被,同时还涉及分子动力学模拟。科学家们的研究结果表明,天然生物聚合物(如壳聚糖、海藻酸钙、果胶、葡聚糖、黄原胶、酪蛋白、明胶、乳清蛋白、玉米醇溶蛋白等)可以修饰脂质载体的外部结构,提高膜的热力学稳定性和抵抗物理化学及机械张力的能力。然而,根据生物活性化合物的类型以及输送系统的设计和生产目标,选择合适的生物聚合物对囊泡的稳定性和载药化合物的生物可及性有重大影响,这是由于储存条件、配方、加工和胃肠道造成的压力所致。

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