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

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.

Updated Information of the Effects of (Poly)phenols against Type-2 Diabetes Mellitus in Humans: Reinforcing the Recommendations for Future Research

“…An alternative strategy to overcome the metabolic transformation that may alter the antidiabetic effects of plant (poly)phenols is to develop new means to deliver these compounds, minimizing their degradation via the use of new engineered delivery systems (nanoparticles) [52]. A wide range of nano-formulations have been investigated and developed to try to maximize the effects of (poly)phenols.…”

Cardioprotective potential of vanillic acid

“…151,152 In addition, nanoencapsulation has been extensively utilized to protect antioxidants from oxidation and lysis by external agents, guaranteeing their stability and enhancing the half-life, bioavailability, and efficacy of active compounds. 153…”

“…Nanoparticles can provide plentiful options for co‐delivering synergistic therapeutic agents by the same nanoparticle 151,152 . In addition, nano‐encapsulation has been extensively utilized to protect antioxidants from oxidation and lysis by external agents, guaranteeing their stability and enhancing the half‐life, bioavailability, and efficacy of active compounds 153 . Nowadays, targeted nanoparticle delivery systems in the field of CVDs are undergoing multiple examinations.…”

Polyphenols–Gut–Heart: An Impactful Relationship to Improve Cardiovascular Diseases

“…The beneficial role of polyphenols towards gut symbiosis and prebiotic effects, as well as antimicrobial activity against pathogenic microflora (both factors exacerbating healthy impacts on the cardiovascular system), needs more experimental and consistent evidence supported by clinical research. The recent biotechnological production of oral formulations of polyphenols in nanocapsules added to foods and beverages, strengthens their delivery in order to treat cardiovascular damage [ 288 ]. However, more in-depth mechanistic knowledge is required for a better understanding of the molecular basis behind polyphenol efficacy in the gut–heart axis, their proper dosage, the absence of side effects, and the necessity of safe formulations that are globally accepted, in addition to the need to obtain unambiguous outcomes from rigorous clinical trials in hospitalized patients.…”