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Engineering oral delivery of hydrophobic bioactives in real-world scenarios
Current Opinion in Colloid & Interface Science ( IF 7.9 ) Pub Date : 2020-03-27 , DOI: 10.1016/j.cocis.2020.03.009
Anwesha Sarkar , Alan R. Mackie

Bioactive compounds, often hydrophobic in nature, tend to degrade during processing outside or inside the body with rapid clearance rates, resulting in poor bioavailability. In this review, we survey recent scientific advances in lipid-based colloidal delivery systems (conventional emulsions/nanoemulsions, Pickering emulsions, multilayered and multiple emulsions, coated/uncoated liposomes, natural microcapsules, and so on) that have been used to improve the bioaccessibility and/or bioavailability of hydrophobic bioactive compounds. Specifically, we use a ‘delivery to design’ approach, that is, we discuss the desired release kinetics of bioactive compounds first. This enables us to paint a more reasonable image of the optimal microstructure sought in the gastrointestinal tract, to lay out the design principles for fabricating the next generation of oral delivery carriers. Finally, we outline the challenges for translation of oral delivery vehicles that show promises in benchtop experiments and how multidisciplinary approaches might help overcoming some of those challenges.



中文翻译:

在实际场景中工程化口服疏水性生物活性物质

生物活性化合物通常是疏水性的,在加工过程中倾向于在体外或体内以快速清除率降解,从而导致不良的生物利用度。在这篇综述中,我们调查了基于脂质的胶体递送系统(常规乳剂/纳米乳剂,Pickering乳剂,多层乳剂和多层乳剂,包衣/未包衣脂质体,天然微胶囊等)的最新科学进展,这些体系已用于改善生物可及性。和/或疏水生物活性化合物的生物利用度。具体而言,我们使用“传递设计”方法,即首先讨论所需的生物活性化合物释放动力学。这使我们能够绘制出更合理的胃肠道最佳显微结构图像,列出制造下一代口服给药载体的设计原则。最后,我们概述了口服递送工具的翻译挑战,这些挑战表明了台式实验的前景,以及多学科方法如何帮助克服其中的一些挑战。

更新日期:2020-03-27
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