Flavonoids through the eyes of a pharmacologist. Features and problems of pharmacokinetics

Abstract

The review focused on pharmacokinetics of the six major subclasses of flavonoids: their distribution, consumption and metabolism. Particular attention is paid to the problem of the bioavailability of these plant polyphenolic compounds, the differences of the effects obtained in experiments in vitro and in vivo. Discusses the dependence of the efficiency of flavonoids by the characteristics of the processes of metabolism in humans. Emphasizes the role of the epithelium of small intestine and microbiota of the colon in ensuring biological activity of flavonoids. (For citation: Zverev YaF. Flavonoids through the eyes of a pharmacologist. Features and problems of pharmacokinetics. Reviews on Clinical Pharmacology and Drug Therapy. 2017;15(2):4-11. doi: 10.17816/RCF1524-11).

Modern Nanocarriers as a Factor in Increasing the Bioavailability and Pharmacological Activity of Flavonoids

“…After absorption, lipophilic aglycones undergo metabolic transformation in the small intestine, liver, and colon. Conjugated products entering the systemic circulation after methylation, sulfation and glucuronization of flavonoids are devoid of the pronounced biological activity characteristic of aglycones in vitro [10,11]. As an example, the blood serum of healthy people, who received 240 mg of flavonolignane silybin, con-Abbreviations: AgNP, argentum-based nanoparticle; AuNP, aurum-based nanoparticle; EGCG, epigallocatechin-3-gallate; HEB, hematoencephalic barrier; GIT, gastrointestinal tract; MSN, silica-based nanoparticle; NLC, nanostructured lipid carrier; PAMAM, polyamidoamine; NS, nanosphere; PAMAM, polyamidoamine; PCL, polycaprolactone; PCR, polymerase chain reaction; PEG, polyethylene glycol; PLA, polylactic acid; PLGA, plyglycolic acid; PNP, polymer nanoparticle; PVP, polyvinylpirrolidone; RES, reticuloendothelial system; ROS, reative oxygen species; SLN, solid lipid nanoparticle.…”