[Influence of resveratrol and dihydroquercetin inclusion into phospholipid nanopatricles on their bioavailability and specific activity].

The effects of natural polyphenols, resveratrol (RES) and dihydroquercetin (DHQ), included in phospholipid nanoparticles, have been compared with free substances of RES and DHQ in in vitro and in vivo experiments. Preincubation of healthy donor plasma low density lipoproteins (LDL) with RES or DHQ included in phospholipid nanoparticles caused a more pronounced decrease in Cu2+ induced lipid oxidation compared with the free substances, and reduced the formation of lipid peroxides products. Bioavailabilities of RES and DHQ in phospholipid formulations after oral administration in rats were increased by 1.5-2 times. In an acute hypoxia model in mice prophylactic two-week administration of RES or DHQ phospholipid formulations resulted in 25% increase in survival and 1.5-fold increase in catalase activity in brain homogenates compared to free substances. Using the model of endothelial dysfunction in rats induced by L-NAME it was shown, that RES markedly attenuated the inhibition effect of L-NAME on NO synthesis. RES in phospholipid nanoparticles had the same action at a dose 10 times lower compared to free RES. Load test with resistance (clamping of the ascending aorta for 30 sec) showed that phospholipid formulation of RES possessed more pronounced protective effect due to the stimulation of endothelial NO-synthase.

[The antiradical activity of plant extracts and healthful preventive combinations of these exrtacts with the phospholipid complex].

Using the chemiluminescence method, the effective concentration of antioxidants (AO) and its reactivity toward peroxyl radicals (ARA, the k7 constant) have been measured for 13 plant extracts. In fact all extracts demonstrated ARA higher than ionol. Larix dahurica, Hypericum perforatum, Potentilla fruticosa, Aronia melanocarpa and Rhaponticum carthamoides extracts showed the highest values of ARA. The combinations Aronia + Raponticum extracts; Larix + Hibiscus extracts; Schizandra +Aronia extracts were synergistic (the synergism effect beta of 38%, 33% and 22%). Apparently this phenomenon is the result of the synergistic interaction between compounds present in plant extracts. The Phospholipid complex--Lipoid S40, lacting any antioxidant effect alone, showed a potent synergistic effect with Aronia extract (beta3 = 60%), Silybum extract (beta3 = 41%). Clinical trials demonstrated, that combinations "Lipoid + Aronia extract", "Lipoid + Larix extract + Hibiscus extract", "Lipoid + Silybum extract", "Lipoid + Q10 + Rosa majalis extract" may be used as an additional component in the medicinal treatment, or as an individual prophylactic agent.

[Bioavailability of oral drug formulations and methods for its improvement].

The recent studies in nanotechnology resulted in the development of novel formulations with improved bioavailability. This is especially important for oral administered drugs as the most convenient formulations. The current review deals with the processes occurring at the gastro-intestinal (GI) tract and their influence on the drug form. The increase of bioavailability of the drug may be achieved through designing novel formulations according to the specific drug properties. They include capsules that release pharmaceutical agents at various parts of the GI tract, floating systems that prolong the presence of the drug in the GI tract, dispersed forms with surface-active soluble polymers, micelles that carry poor-soluble drugs inside their non-polar core, agents that facilitate tight junction opening, such as caprate and chitosan, and lipid-based formulations. The own data show the stimulating influence of phospholipid nanoparticles on peroral absorption of drug indomethacin in rats and on passage of transport marker and drugs through Caco-2 cell monolayer in vitro. The review summarizes current understanding of factors that influence the bioavailability of the oral drug forms, currently used models for pharmacokinetic studies, and various approaches to developing novel pharmaceutical forms that increase the bioavailability of the drugs.

[Biological activity of linseed oil as the source of omega-3 alpha-linolenic acid]. / Biologicheskaia aktivnost' l'nianogo masla kak istochnika omega-3 al'fa-linolenovoi kisloty.

Flaxseed oil is the most abundant plant source of omega-3 fatty acid, alpha-linolenic acid omega-3. This review focuses on the biological effects of dietary alpha-linolenic acid (ALA) compared with long-chain omega-3 derivatives. ALA is not equivalent in its biological effects to the long-chain omega-3 fatty acids found in marine fish oils. However, ALA is metabolized to eicosapentaenoic acid, which may replace arachidonic acid in membrane phospholipides. Ingestion of flaxseed oil may alter the generation of eicosanoids, procoagulant activity and other membrane-dependent responses and exert antiallergic, antiatherosclerotic, antiarrhythmic effects. Beneficial effects of flaxseed oil have been shown in prevention and management of cardiovascular disease.

[Biological effects of the soybean phospholipids]. / Biologicheskaia aktivnost' soevykh fosfolipidov.

Soyabean phospholipids, particularly commercial lecithin, are now widely used as biological active food additives. Mechanisms of their activities are based mainly on their similarity with ow phospholipids of biomembranes and blood lipoproteins. The similarity allows the inclusion of plant phospholipids into these structures and promotes prevention of number of pathological processes. Soybean phospholipids have a wide range of biochemical and physical effects. Lecithin complex is the source of easily accessible linoleic acid, choline and inositol. Lecithin plays a notable role as synergist for antioxidants also. The proven health benefits which can be achieved by taking soybean phospholipids include lipid-lowering; control of blood levels of cholesterol and triglyceride, stabilisation of the membrane functions, supporting the hepatic functions. Structure, some physico-chemical properties and metabolism of phospholipids, and molecular mechanisms of their prophylactic effects are briefly reviewed.