Increasing the Power of Polyphenols through Nanoencapsulation for Adjuvant Therapy against Cardiovascular Diseases

Molecules. 2021 Jul 30;26(15):4621. doi: 10.3390/molecules26154621.

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.

Keywords: antioxidants; bioavailability; cardiovascular health; nanocarriers; polyphenol-loaded nanoparticles; pre-clinical trials.

Publication types

  • Review

MeSH terms

  • Antioxidant Response Elements
  • Antioxidants / chemistry
  • Antioxidants / pharmacokinetics
  • Antioxidants / pharmacology*
  • Arginine / analogs & derivatives
  • Arginine / antagonists & inhibitors
  • Arginine / metabolism
  • Cardiotonic Agents / chemistry
  • Cardiotonic Agents / pharmacokinetics
  • Cardiotonic Agents / pharmacology*
  • Diabetes Mellitus / drug therapy
  • Diabetes Mellitus / genetics
  • Diabetes Mellitus / metabolism
  • Diabetes Mellitus / physiopathology
  • Drug Carriers
  • Drug Compounding / methods*
  • Dyslipidemias / drug therapy
  • Dyslipidemias / genetics
  • Dyslipidemias / metabolism
  • Dyslipidemias / physiopathology
  • Gene Expression Regulation / drug effects
  • Humans
  • Hypertension / drug therapy*
  • Hypertension / genetics
  • Hypertension / metabolism
  • Hypertension / physiopathology
  • Myocardial Ischemia / drug therapy*
  • Myocardial Ischemia / genetics
  • Myocardial Ischemia / metabolism
  • Myocardial Ischemia / physiopathology
  • NF-E2-Related Factor 2 / genetics
  • NF-E2-Related Factor 2 / metabolism
  • Nanocapsules / administration & dosage
  • Nanocapsules / chemistry
  • Nitric Oxide / antagonists & inhibitors
  • Nitric Oxide / biosynthesis
  • Oxidative Stress / drug effects
  • Polyphenols / chemistry
  • Polyphenols / pharmacokinetics
  • Polyphenols / pharmacology*
  • Signal Transduction

Substances

  • Antioxidants
  • Cardiotonic Agents
  • Drug Carriers
  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • Nanocapsules
  • Polyphenols
  • Nitric Oxide
  • N,N-dimethylarginine
  • Arginine