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提高白藜芦醇全身及局部生物利用度的策略:最新进展

Strategies to Improve Resveratrol Systemic and Topical Bioavailability: An Update.

作者信息

Intagliata Sebastiano, Modica Maria N, Santagati Ludovica M, Montenegro Lucia

机构信息

Department of Drug Sciences, University of Catania, 95125 Catania, Italy.

出版信息

Antioxidants (Basel). 2019 Jul 25;8(8):244. doi: 10.3390/antiox8080244.

Abstract

In recent years, a great deal of attention has been paid to natural compounds due to their many biological effects. Polyphenols are a class of plant derivatives that have been widely investigated for preventing and treating many oxidative stress-related pathological conditions, such as neurodegenerative and cardiovascular diseases, cancer, diabetes mellitus and inflammation. Among these polyphenols, resveratrol (RSV) has attracted considerable interest owing to its high antioxidant and free radical scavenging activities. However, the poor water solubility and rapid metabolism of RSV lead to low bioavailability, thus limiting its clinical efficacy. After discussing the main biochemical mechanisms involved in RSV biological activities, this review will focus on the strategies attempted to improve RSV effectiveness, both for systemic and for topical administration. In particular, technological approaches involving RSV incorporation into different delivery systems such as liposomes, polymeric and lipid nanoparticles, microemulsions and cyclodextrins will be illustrated, highlighting their potential clinical applications. In addition, chemical modifications of this antioxidant aimed at improving its physicochemical properties will be described along with the results of in vitro and in vivo studies.

摘要

近年来,由于天然化合物具有多种生物学效应,因此受到了广泛关注。多酚是一类植物衍生物,已被广泛研究用于预防和治疗许多与氧化应激相关的病理状况,如神经退行性疾病、心血管疾病、癌症、糖尿病和炎症。在这些多酚中,白藜芦醇(RSV)因其高抗氧化和自由基清除活性而备受关注。然而,RSV的水溶性差和代谢迅速导致其生物利用度低,从而限制了其临床疗效。在讨论了RSV生物活性所涉及的主要生化机制后,本综述将重点关注为提高RSV全身和局部给药有效性而尝试的策略。特别是,将阐述涉及将RSV掺入不同递送系统(如脂质体、聚合物和脂质纳米颗粒、微乳液和环糊精)的技术方法,突出其潜在的临床应用。此外,还将描述旨在改善该抗氧化剂物理化学性质的化学修饰以及体外和体内研究结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fa84/6719186/276618d299f6/antioxidants-08-00244-g001.jpg

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