Abstract
Polyphenols play a therapeutic role in vascular diseases, acting in inherent illness-associate conditions such as inflammation, diabetes, dyslipidemia, hypertension, and oxidative stress, as demonstrated by clinical trials and epidemiological surveys. The main polyphenol cardioprotective mechanisms rely on increased nitric oxide, decreased asymmetric dimethylarginine levels, upregulation of genes encoding antioxidant enzymes via the Nrf2-ARE pathway and anti-inflammatory action through the redox-sensitive transcription factor NF-κB and PPAR-γ receptor. However, poor polyphenol bioavailability and extensive metabolization restrict their applicability. Polyphenols carried by nanoparticles circumvent these limitations providing controlled release and better solubility, chemical protection, and target achievement. Nano-encapsulate polyphenols loaded in food grade polymers and lipids appear to be safe, gaining resistance in the enteric route for intestinal absorption, in which the mucoadhesiveness ensures their increased uptake, achieving high systemic levels in non-metabolized forms. Nano-capsules confer a gradual release to these compounds, as well as longer half-lives and cell and whole organism permanence, reinforcing their effectiveness, as demonstrated in pre-clinical trials, enabling their application as an adjuvant therapy against cardiovascular diseases. Polyphenol entrapment in nanoparticles should be encouraged in nutraceutical manufacturing for the fortification of foods and beverages. This study discusses pre-clinical trials evaluating how nano-encapsulate polyphenols following oral administration can aid in cardiovascular performance.
Highlights
Natural bioactive agents are attractive molecules, as their implicit safe status allows them to be tested as specific or multiple target regulators in signaling or functional human pathways, while comprising promising therapeutic adjuvant candidates against multifactorial and complex physiopathological conditions, including degenerative diseases and metabolic dysfunctions
Oxidative stress is a physiopathological condition enrolled in risk factors for cardiovascular diseases, and the monitoring of end products generated from the oxidation of biological macromolecules in biological fluids as well as intracellular antioxidant enzyme levels are used to assess the degree of cell damage and the therapeutic potential of drugs and bioactive compounds [177]
Polyphenol effectiveness depends on antioxidant characteristics, which requires that their chemical structure be preserved along the gastrointestinal tract during intestinal absorption, when in the bloodstream, when reaching the target cell these compounds, and when crossing plasmatic or intracellular membranes in order to exert their bioactivity
Summary
Natural bioactive agents are attractive molecules, as their implicit safe status allows them to be tested as specific or multiple target regulators in signaling or functional human pathways, while comprising promising therapeutic adjuvant candidates against multifactorial and complex physiopathological conditions, including degenerative diseases and metabolic dysfunctions. As a carrier system for therapeutic agents, nanoparticles can provide a controlled release of the active principle after oral, parenteral, or topical administration and, at the same time, guarantee better solubility and chemical structure stability, ensuring target achievement [33] Due to their subcellular size similar to biomolecules, NPs are able to pass through the pores of the intestinal epithelium, cross biological barriers, including the blood-brain barrier, and penetrate tissues through microcapillaries, allowing for the delivery of therapeutic agents to specific organs and tissues and resulting in greater bioavailability [34,35,36,37,38,39,40]. The current framework concerning possible polyphenol gastrointestinal toxicity, bioavailability, and bioactivity addressed through clinical trials is reviewed and, the projection of the performance of nano-encapsulated polyphenols in aiding cardiovascular impairments is discussed
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