[Interaction of rifampicin embedded in phospholipid nanoparticles with blood plasma lipoproteins].

The drug formulations of antituberculous remedy rifampicin in nanoparticles less than 30 nm based on soy phosphatidylcholine and sodium oleate was elaborated in Institute of Biomedical Chemistry. The distribution of rifampicin in blood plasma fractions after incubation with this formulation and with free rifampicin was studied. This goal was stimulated by the literature data about activation of macrophages LDL receptors in cases of M.

[Nanoparticles as drug delivery system for antituberculous drugs].

The increase of tuberculosis incidence in last decade stimulated elaboration of both new antituberculous drugs and also searches ofoptimiting delivery systems for existing drugs. It is determined by their side effects and low bioavailability of effective first line drug rifampicin. Various nanosystems for transport of antituberculous drugs are considered on the basis of various polymers, liposomes, lipid nanoparticles, nanoemulsios, nanosuspensions, dendrimers, cyclodextrines.

[The increase of bioavailability and anti-inflammatory effect of indomethacin loaded into phospholipid nanoparticles].

The ultrafine formulation on the base of plant phosphatidylcholine and antiinflammatory remedy indomethacin with nanoparticles less than 50 nm was obtained. Drug bioavailability after its peroral administration to rats was more than 2 fold higher as compared with free indomethacin. Increased antiinflammatory activity of indomethacin in phospholipids nanoparticles as compared with its free form was shown in two models of inflammation - adjuvant arthritis in rats and conconavalin A induced edema in mice.

[Changes of doxorubicin distribution in blood and plasma after its inclusion into nanophospholipd formulation].

The drug composition based on the plant phospholipids and the antitumor drug doxorubicin (particle size <30 nm) was obtained using original technology elaborated in the Institute of Biomedical Chemistry (Russian Academy of Medical Sciences). In in vitro experiments demonstrated decreased drug association with blood cells for this nanophospholipid form as compared with free doxorubicin. This was accompanied by a with corresponding increase in its plasma level ans also by drug redistribution from plasma protein fraction to high density lipoproteins.

[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.

[Plasma lipoproteins as drug carriers. Effect of phospholipid formulations].

The extensive development of nanotechnologies in the last two decades has brought about new understanding of plasma lipoproteins (LP) as natural drug nanocarriers that escape interaction with immune and reticuloendothelial systems. Drugs bound to LP (especially LDL) can more actively penetrate into cells of many cancer and inflammation tissues with enhanced expression or/and dysregulation of B,E receptors or possibly scavenger SR-BI receptors. Relevant studies are focused on the development of new dosage forms by conjugating lipophilic drugs either with isolated plasma LP or with their model formulations, such as nanoemulsions, mimetics, lipid nanospheres, etc.

[Comatose states: etiopathogenesis, experimental studies, treatment of hepatic coma].

The review presents the modern concepts on biochemical mechanisms of processes, that result in comatose states (CS), with emphasis on the search of new therapeutic approaches. CS of various origin causes severe suppression of brain cells functioning and stable unconsciousness. Numerous reasons of various CS are classified into two main groups: primary brain damages (ischemia, tumor, trauma) and secondary damages originating from system injuries in the body (endocrine, toxic e.

[Possibilities for use of phospholipid nanosystem with glycyrrhizic acid ("phosphogliv") for optimization of drugs: doxorubicin and budesonide as examples].

The complexes of phospholipids nanoparticles (as the injection form of newly developed hepatoprotector phosphogliv) with the antitumor drug doxorubicin or with glucocorticoid budesonide have been investigated for their pharmacological activity in comparison with free forms of these drugs. Doxorubicin with phosphogliv revealed more antitumor and antimetastatic activity in C47B 1/6 mice with carcinoma LLC than free doxorubicin. Inhalation of budesonide with phosphogliv in vivo to quinea pigs resulted to more pronounced decrease of antigen or histamin induced bronchospasm, particularly its subacute phase, as compared with traditional powder or suspension budesonide forms.

[Antirheumatoid activity of methotrexate in phospholipid nanoparticles (Phosphogliv)].

The efficiency of methotrexate use in basic therapy of rheumatoid arthritis is limited because of risk of side effects and fast drug efflux from zone of joints as well. The new stabilized form of methotrexate was elaborated with phospholipid micelles as a carrier. The injective form of the preparation Phosphogliv was used for this purpose.

[Membrane proteins and phospholipids as effectors of reverse cholesterol transport].

The review highlights the membrane aspect of cholesterol efflux from cell membranes to high density lipoproteins (HDL), an initial stage of reverse cholesterol transport to liver. Special attention is paid to ABC-A1 transporter and membrane SR-B1 receptor, their properties, putative mechanisms of action and their role in reverse cholesterol transport. Interaction of ABC-AI with plasma free apoA1 is suggested to facilitate the efflux of membrane phospholipids and formation of their complex with apoAI.

[Hemorheological and clinical efficiency of a new phospholipid hepatoprotective drug Phosphogliv in patients with psoriatic arthritis].

A new phospholipid drug "Posphogliv" showed earlier good results in the treatment of liver discases. The mechanism of its effect consists in non-specific repair of biomembranes. In the present study it was used for the treatment of in patients with psoriatic arthritis, accompanied by severe damages of blood rheology.

[The way of evaluation of cholesterol accepting capacity of plasma high density lipoproteins].

The simple way of quantitative evaluation of high density lipoproteins (HDL) capacity to absorb additive cholesterol quantity is proposed. It allows to evaluate indirectly intensity of the first, rate limiting stage of reverse cholesterol transport its accepting from the cells by means of HDL. The way includes the usage of stable artificial cholesterol donor--cholesterol covered inert polymer particles, which are than more convenient, than cell culture use.

[Hypolipoproteinemia and secondary role of atherosclerosis in the development of ischemic heart disease in patients with polycythemia vera].

Relationship between presence of coronary heart disease (CHD), coronary risk factors (parameters of lipid transport system and hypertension) and disturbances of microcirculation was studied in patients with myeloproliferative blood disease Polycythemia Vera (PV). Probability of tissue (including blood vessel wall) cholesterol accumulation was estimated by measurement of its content in skin surface layers. PV patients (n=55, including 27 patients with CHD) had predominant hypolipoproteinemia with normal proportion of various lipoprotein classes.

[Biological effects of the soybean phospholipids].

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.

[Phosphatidylcholine as the basis for artificial pulmonary surfactants: comparison of surface active properties].

The Wilhelmy balance was used for in vitro testing of surface active properties of natural phosphatidylcholines (PCs) as possible basis for surfactant replacement therapy. Saturated PC, dipalmitoylphosphatidylcholine (DPPC) and phospholipon (PL) had similar parameters of surface activity: minimal values of equilibrium surface tension (EST) and the longest surface spreading time (SST). Unsaturated egg and soybean PCs also shared similar values of surface activity parameters (EST and SST).

[Relation between resistance to oxidation and cholesterol acceptance of high density lipoproteins in patients with ischemic heart disease].

Cholesterol (CH) acceptance ability of high density lipoproteins (HDL) was assessed in 43 ischemic heart disease (IHD) patients, including patients with post-infarction cardiosclerosis and class II-III effort angina. CH acceptance ability of HDL was measured as increment of HDL CH after incubation with artificial CH-containing system. Oxidabilities of HDL and total plasma were estimated by quantitation of lipid peroxidation products (hydroperoxides and thiobarbituric acid-reactive substances - TBARS) after incubation with Cu(2+) ions.

[Erythrocyte cholesterol content in polycythemia vera: relation to ischemic heart disease].

Relative cholesterol content and its distribution between erythrocytes and plasma were studied in 34 patients with polycythemia vera (PV) both with and without concomitant coronary heart disease (CHD). Deformability of erythrocytes, disturbances of microcirculation (blood flow fragmentation, decrease of capillary density) were also assessed. Erythrocytes cholesterol/phospholipids molar ratios (0.

[Characteristics of the lipid transport system in psoriasis].

Cholesterol of high density lipoprotein (HDL) subfractions (HDL2 and HDL3), activity of cholesterol ester transport protein (CETP), and standard lipoprotein parameters (cholesterol, triglycerides, HDL cholesterol) were measured in plasma of 192 patients with various psoriasis forms, which included simple "distributed psoriasis", erythrodermic and arthropathic psoriasis. Among psoriatic patients unusually high percent of persons with both hypo- and hyper-cholesterolemia was observed. The same situation was observed with frequency of cases with both low and high plasma HDL cholesterol levels, the distribution being depending from disease severity.

[Phosphogliv: mechanism of therapeutic action and clinical efficacy].

The review summarizes the results of long term study (from design to clinical trial) of a new hepatoprotective drug Phosphogliv. Some theoretical ground for its creation has been considered with special emphasis on its ingredient properties: soy bean phosphatidylcholine and glycyrrhizinic acid from licorice roots. Experimental and clinical data concerning polyene phosphatidylcholine repairing action on cell membranes as well as antiviral and immunomodulating effects of glycyrrhizinic acid are presented.

[New domestic phospholipid preparation "Fosfogliv" as an effective treatment for patients with acute viral hepatitis].

Patients with acute viral hepatitis B, A and mixed hepatitis B + C were treated in two independent clinics with phosphogliv--a new hepatoprotective drug based on polyunsaturated phosphatidylcholine and glycyrrhizic acid salt. Phosphogliv removed some symptoms of intoxication (nausea, weakness, jaundice, etc.) quicker than basic therapy.

[Hepatoprotective action of phosphogliv in surgery of patients with chronic calculous cholecystitis].

32 patients with chronic calculous cholecystitis were treated by a new preparation. Phosphogliv (on the base of polyunsaturated phospholipids)--5 days before planned surgery and 5 days after. The increase of alanine and asparagine aminotransferases activities and of bilirubin concentration (2-2.

[Comparative study of the effects of essentiale and the novel Russian hepatoprotective agent "phospholiv" in a model of acute hepatitis in rats].

Curative effect of new preparation "Phospholiv", elaborated in Institute of Biomedical Chemistry, in acute CCl4 induced rat hepatit model was studied. The preparation consists of polyunsaturated phosphatidylcholine and glycyrrhizinic acid salt. Recovery of damaged biosynthesis of albumin and total cell liver RNA--by incorporation of C14-leucine and C14-orotic acid--were observed after 3 days Phospholiv administration, that showed on reparation of damaged protein-synthesis system.

[Use of a novel hepato-protective preparation "phospholiv" for inhibition of development of chronic hepatitis in rats].

Protective influence of a new phospholipid preparation "Phospholiv" was studied using a model of chronic hepatitis. Animals were treated 45 days intraperitoneay with CCl4 with parallel intragastral administration of Phospholiv or--(for comparison)--the of other phospholipid hepatoprotector, Essential. Morphologic changes of liver, as well as protein and RNA biosynthesis were evaluated in the end of experiment--by means of measuring C14-leucine and C14-orotic acid incorporation into hepatocyte subcellular fractions.

[Features of distribution of free and esterified cholesterol in the epidermis, biological membranes and plasma lipoproteins in psoriasis].

The parameters of cholesterol (CS) metabolism in the epidermis, blood plasma lipoproteins, and red cell membranes were assessed in patients with psoriasis. The levels of free and total CS in extracts from the surface of epidermis, in plasma lipoproteins, and in plasma triglycerides were measured, and the molar ratio CS/ phospholipids (CS/PL index) in red cell membranes assessed in 194 patients with psoriasis of different severity. The levels of free and total CS in the epidermis were found to increase as the psoriatic process grew in severity.