Biocompatible nanoparticles with enhanced therapeutic efficacy of flavonoids in food
Flavonoids have a key role in plant growth and development and their protection from all kinds of environmental stress like UV radiation, heat, coldness and numerous parasites. Flavonoids as catalysts of electron transport affect photosynthesis, ionic channels and vacuolar transport. In spite of their extraordinary therapeutic potential as was demonstrated in vitro, their use is nevertheless very limited because of low solubility in water and fast metabolic degradation in organism. Bioavailability of quercetin when applied orally is only 1% in humans. When applied intravenously, from the initial concentration of 100 mg in plasma, after 3 hours only micromolar concentrations are present. Flavonoid loading of nanoparticles (NP) could significantly improve the oral administration of flavonoids, protecting them from degradation in digestive tract. In addition, extended release of the active substance could be ensured by their oral and parenteral administration. In order to fulfill these requirements, NP must also be stable enough. Two groups of NP having been investigated for that purpose are inorganic and organic NP. However, neither one of them possesses the wanted properties.
The goal of this project is preparation of a functional prototype of biodegradable NP having built-in flavonoids as an original solution up to date not present on the market. Such NP would have a capacity of flavonoid integration greater then presently achieved 2 % of NP mass and ability of controllable release in physiological conditions. They are also expected to be a solution to the problem of chemical instability of flavonoids and their low solubility in water. Specifically, the activity of two flavonols, myricetin and myricitrin, will be investigated. Myricetin exhibits anti-tumor and anti-inflammatory effects with strong activity in radical scavenging. Myricitrin exhibits an extraordinary antioxidative, anti-inflammatory and anti-nociceptive activity in numerous cells. As a reference quercetin will be used. There are two possible types of projects risks: a) NP will not possess the expected capacity of flavonoid adsorption and b) NP loaded with flavonoids will not release them in satisfactory rate.
Project team has eight members including principal investigator, six researchers and two postdoctoral researchers. The RBI team possesses experience in preparation of a whole suite of model membrane systems of increasing complexity. Team has expertise in colloid and interface chemistry, including testing of NPs stability in different media, determining drug release kinetics, and in the application of different techniques (AFM and FS), FTIR and ATR spectroscopy.
Goran Baranović, PhD, Scientific Advisor, retired