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植物源抗氧化剂递释的纳米制剂方法进展:以槲皮素为例。

Advances on nanoformulation approaches for delivering plant-derived antioxidants: A case of quercetin.

机构信息

UKA Tarsadia University, Maliba Pharmacy College, Gopal-Vidyanagar Campus, Surat 394350, India.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER) - Raebareli, Lucknow 226002, India.

出版信息

Int J Pharm. 2022 Sep 25;625:122093. doi: 10.1016/j.ijpharm.2022.122093. Epub 2022 Aug 8.

Abstract

Oxidative stress has been implicated in tumorigenic, cardiovascular, neuro-, and age-related degenerative changes. Antioxidants minimize the oxidative damage through neutralization of reactive oxygen species (ROS) and other causative agents. Ever since the emergence of COVID-19, plant-derived antioxidants have received enormous attention, particularly in the Indian subcontinent. Quercetin (QCT), a bio-flavonoid, exists in the glycosylated form in fruits, berries and vegetables. The antioxidant potential of QCT analogs relates to the number of free hydroxyl groups in their structure. Despite presence of these groups, QCT exhibits substantial hydrophobicity. Formulation scientists have tested nanotechnology-based approaches for its improved solubilization and delivery to the intended site of action. By the virtue of its hydrophobicity, QCT gets encapsulated in nanocarriers carrying hydrophobic domains. Apart from passive accumulation, active uptake of such formulations into the target cells can be facilitated through well-studied functionalization strategies. In this review, we have discussed the approaches of improving solubilization and bioavailability of QCT with the use of nanoformulations.

摘要

氧化应激与肿瘤形成、心血管、神经和与年龄相关的退行性变化有关。抗氧化剂通过中和活性氧 (ROS) 和其他致病因子来最小化氧化损伤。自 COVID-19 出现以来,植物来源的抗氧化剂受到了极大的关注,特别是在印度次大陆。槲皮素 (QCT) 是一种生物类黄酮,以糖苷的形式存在于水果、浆果和蔬菜中。QCT 类似物的抗氧化潜力与其结构中游离羟基的数量有关。尽管存在这些基团,QCT 仍表现出显著的疏水性。制剂科学家已经测试了基于纳米技术的方法来提高其溶解度并将其递送到预期的作用部位。由于其疏水性,QCT 被包裹在带有疏水区的纳米载体中。除了被动积累外,通过经过充分研究的功能化策略,可以促进此类制剂主动进入靶细胞。在这篇综述中,我们讨论了使用纳米制剂来提高 QCT 的溶解度和生物利用度的方法。

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