Nanoformulations to Enhance the Bioavailability and Physiological Functions of Polyphenols

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molecules Review Nanoformulations to Enhance the Bioavailability and Physiological Functions of Polyphenols Bingyan Yang, Yixin Dong, Fei Wang and Yu Zhang * Jiangsu Provincial Key Lab for the Chemistry and Utilization of Agro-Forest Biomass, Jiangsu Key Lab of Biomass-Based Green Fuels and Chemicals, Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China; taylor1106@163.com (B.Y.); kaydong417@163.com (Y.D.); hgwf@njfu.edu.cn (F.W.) * Correspondence: yuzhang@njfu.edu.cn; Tel.: +86-25-8542-7635; Fax: +86-25-8541-8873 Academic Editor: Paola Di Donato and Brigida Silvestri Received: 16 September 2020; Accepted: 6 October 2020; Published: 10 October 2020 􏰁􏰂􏰃 􏰅􏰆􏰇 􏰈􏰉􏰊􏰋􏰌􏰂􏰍 Abstract: Polyphenols are micronutrients that are widely present in human daily diets. Numerous studies have demonstrated their potential as antioxidants and anti-inflammatory agents, and for cancer prevention, heart protection and the treatment of neurodegenerative diseases. However, due to their vulnerability to environmental conditions and low bioavailability, their application in the food and medical fields is greatly limited. Nanoformulations, as excellent drug delivery systems, can overcome these limitations and maximize the pharmacological effects of polyphenols. In this review, we summarize the biological activities of polyphenols, together with systems for their delivery, including phospholipid complexes, lipid-based nanoparticles, protein-based nanoparticles, niosomes, polymers, micelles, emulsions and metal nanoparticles. The application of polyphenol nanoparticles in food and medicine is also discussed. Although loading into nanoparticles solves the main limitation to application of polyphenolic compounds, there are some concerns about their toxicological safety after entry into the human body. It is therefore necessary to conduct toxicity studies and residue analysis on the carrier. Keywords: polyphenols; bioavailability; loading; nanoformulations 1. Introduction Many effective medical treatments have originated from plant extracts, which are important sources of materials for the treatment of many diseases [1]. Phenolic compounds are widely present as secondary metabolites in all vascular plants [2–5]. They play important roles in the growth and development of plants, and are involved in defense against ultraviolet light and pathogens [6]. In recent years, because of their potential positive role in human metabolism, they have attracted increasing attention and research. These compounds have biological properties that include antioxidant, anti-inflammatory, antibacterial, anticancer and cardiovascular protection activities [7–9]. However, the use of phenolic compounds in humans is limited by many factors, such as low solubility, poor permeability, instability, rapid release, susceptibility to environmental influences and low bioavailability [10,11]. In order to overcome these limitations, polyphenols are often loaded into various carriers to enhance their bioavailability. This can increase biocompatibility, prevent degradation caused by the external environment, and prevent interaction with other components in the human body. Nanocarriers have been demonstrated to be excellent materials for encapsulating phenolic compounds and improving their bioavailability. With the rapid development of nanotechnology in the food and pharmaceutical industries, many advanced nanoparticles have been developed to protect and control/target the release of biologically active ingredients, including various polyphenols [12–15]. The size of nanoparticles and Molecules 2020, 25, 4613; doi:10.3390/molecules25204613 www.mdpi.com/journal/molecules

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