Assessing the effectiveness of fenbendazole supramolecular complexes against schistosomiasis, monieziosis and parabronemosis in sheep.

Helminth infections pose a significant economic threat to livestock production, causing productivity declines and, in severe cases, mortality. Conventional anthelmintics, exemplified by fenbendazole, face challenges related to low solubility and the necessity for high doses. This study explores the potential of supramolecular complexes, created through mechanochemical modifications, to address these limitations.

Synthesis and Clinical Examination of Novel Formulations of Ivermectin, Albendazole and Niclosamide for the Treatment of Equine Gastrointestinal Helminthoses.

Background: This study aimed to develop new complex preparations of ivermectin, niclosamide and albendazole based on solid-phase mechanochemical technology, and to evaluate their efficacy against equine nematodosis and cestodosis.

Methods: Novel formulation of antiparasitic paste were prepared using joint mechano-chemical treatment of ivermectin (0.2 mg/kg bodyweight; BW), niclosamide (10 mg/kg BW) and albendazole (3, 5, 10 mg/kg BW) substances with polyvinylpyrrolidone and arabinogalactan.

Efficacy of Novel Formulations of Ivermectin and Albendazole in Parasitic Infections of Sheep in the Altai Mountains of Russia.

Background: Parasitic infections are widespread in sheep farms of the Russian Federation, including Siberia. The infection of sheep with helminths and parasitic arthropods with a range of 70% to 100% in different regions, contributes to a decrease in the productivity and quality of products, and even death of animals. This study aimed to formulate drugs with pronounced parasiticidal effects based on ivermectin and albendazole, widely used to treat animal entomoses and helminth infections.

Pharmacokinetic profile, tissue residue depletion and anthelmintic efficacy of supramolecular fenbendazole.

A supramolecular complex of fenbendazole (SFBZ) with polyvinylpyrrolidone (PVP) was created by mechanochemical processing to increase its anthelmintic efficacy and to reduce the dose of applied drugs. The aim of our research was to study the pharmacokinetic profile and tissue residue depletion of fenbendazole (FBZ) and its metabolites: sulfoxide and sulfone in sheep after SFBZ treatment by high-performance liquid chromatography with tandem mass spectrometric detection and to evaluate its efficacy against gastrointestinal strongylatosis of sheep in field trials. The results revealed that FBZ and its metabolites were detected in blood serum in 2 h after SFBZ administration and in 4-6 h after the administration of the basic - FBZ.

Innovative anthelmintic based on mechanochemical technology and their efficacy against parasitic infection of sheeps.

Objective: Solubility and bioavailability are crucial for maximizing the activity of an antiparasitic drug. This study aimed to develop a combined preparation for antiparasitic medicines using ivermectin (Iver), fenbendazole (FBZ), and triclabendazole (TBZ), considering their solubility, bioavailability, and activity.

Materials And Methods: Innovative preparations in solid dispersions (SD) were obtained using the joint mechanical processing of drug substances with polyvinylpyrrolidone (PVP) in an LE-101 roller mill.

Anthelmintic Efficacy of Supramolecular Complex of Praziquantel Obtained by Mechanochemical Technology.

Background: A supramolecular complex of praziquantel (PZQ) with disodium salt of glycyrrhizic acid (NaGA) was obtained by mechanochemical technology to increase solubility, absorption rate and hence bioavailability of the drug and reduction its therapeutic doses. The aim of our study was evaluation of anthelmintic efficacy of supramolecular complex of PZQ.

Methods: Different samples of PZQ with NaGA were obtained by mechanochemical processing and examined for some physico-chemical properties.

Glycyrrhizin-induced changes in phospholipid dynamics studied by H NMR and MD simulation.

Phospholipid bilayer constitutes the basis of the cell membrane. Any changes in its structure and dynamics could significantly affect the properties and functions of the cell membrane and associated proteins. It could, in its turn, affect the mechanism and strength of drug-membrane interaction.

Arabinogalactan and glycyrrhizin based nanopesticides as novel delivery systems for plant protection.

During the past decade, nanotechnologies opened a new era in delivery of plant protection products through the development of nanosized controlled release systems, such as polymer nanoparticles, micelles, and so on using a wide variety of materials. To increase the pesticides penetration into the grain under the presowing seed treatment, a new approach based on non-covalent associate preparation with natural polysaccharides and oligosaccharides as delivery systems (DSs) was applied. Earlier, this approach was tested on antidote 1,8-naphthalic anhydride (NA).

Influence of mechanochemical technology on anthelmintic efficacy of the supramolecular complex of fenbendazole with polyvinylpyrrolidone.

Objective: The purpose of our research was to evaluate the effect of mechanochemical technology on the efficacy of supramolecular complex of fenbendazole (SMCF) with polyvinylpyrrolidone (PVP) polymer against some helminthosis of animals.

Materials And Methods: The SMCF samples with PVP were synthesized using a solid-state mechanochemical technology in activators of impact-abrading type and their physicochemical properties were analyzed. The efficacy of SMCF was studied on the laboratory model of and infection of mice and helminthosis of sheep.

The efficacy of the supramolecular complexes of niclosamide obtained by mechanochemical technology and targeted delivery against cestode infection of animals.

Niclosamide is an anthelmintic that is widely used to treat cestode infection of animals. The efficacy of the supramolecular complexes of niclosamide obtained by mechanochemical technology and targeted delivery was studied in hymenolepiosis of mice and monieziosis of sheep. The efficacy of new substances of niclosamide with polyvinylpyrrolidone polymer in different ratios (1:10; 1:5; 1:2) was determined by the results of helminthological necropsy of the small intestine of sheep and mice.

Natural Poly- and Oligosaccharides as Novel Delivery Systems for Plant Protection Compounds.

To increase the bioavailability of plant protection products, we have applied a new approach based on noncovalent association with natural water-soluble polysaccharides and oligosaccharides as delivery systems (DSs). The mechanochemical technique has been applied to prepare the solid-state nanodispersed compositions of antidote 1,8-naphthalic anhydride (NA) with arabinogalactan, sodium salt of carboxymethylcellulose, and glycyrrhizin as DSs. The effect of DSs on the solubility and the penetration of NA into the seeds of barley and wheat has been investigated by various physicochemical techniques.

Spectroscopic and molecular dynamics characterization of glycyrrhizin membrane-modifying activity.

Glycyrrhizic acid (GA) is a triterpene glycoside extracted from licorice root. Due to its amphiphilicity GA is capable of forming complexes with a variety of hydrophobic molecules, substantially increasing their solubility. GA can enhance the therapeutic effects of various drugs.

A Physicochemical and Pharmacological Study of the Newly Synthesized Complex of Albendazole and the Polysaccharide Arabinogalactan from Larch Wood.

Inclusion complexes of albendazole (ABZ) with the polysaccharide arabinogalactan from larch wood Larix sibirica and Larix gmelinii were synthesized using a solid-state mechanochemical technology. We investigated physicochemical properties of the synthesized complexes in the solid state and in aqueous solutions as well as their anthelmintic activity against Trichinella spiralis, Hymenolepis nаna, Fasciola hepatica, Opisthorchis felineus, and mixed nematodoses of sheep. Formation of the complexes was demonstrated by means of intrinsic solubility and the NMR relaxation method.

[Efficacy of a new fenbendazole formulation produced by nanotechnology-based drug delivery system against nematodosis].

The efficacy of a new fenbendazile formulation produced by nanotechnology-based drug delivery system was investigated in45 sheep naturally infected with gastrointestinal nematodes. The formulation showed 95.6% efficacy against Nematodes spp.

[The effect of the dispersity of tegalid on its bioavailability].

The impact of the new helminthicide Tegalide, a dibromobenzamide derivative, on its pharmacology was investigated. The agent given as a fine-dispersed form was found to be more intensively absorbed by the body and to be in animals' blood for a longer period of time (MRT fine-dispersed and MVR coarse-dispersed were 88.5 and 50.

[Synthesis and biological activity of new analogs of beta-casomorphine-5].

Four new analogues of beta-cazomorphine-5 modified at the C-end with ethylenediamine- and glycine-containing derivatives were synthesized by the standard method of peptide chemistry (mixed anhydrides, carbodiimide, activated esters): H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-II (I) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-II (II) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-CO-CH3 (III) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-CO-CH2-CH2-COOH (IV) The level of affinity and the degree of selectivity of the peptides towards the mu- and delta-opioid receptors of the rat brain lyophilized membranes were studied by the radioreceptor method. All the new peptides displayed analgetic activity, largely depending upon their structure.

[Synthesis of new fragments of VP1 protein fragments from foot and mouth disease virus type A22. Synthesis of fragments 134-139, 134-145, 140-145, 150-155, and 150-159].

Fragments 134-145 and 150-159 of the antigenic-region of the VP1 protein of the A22 foot-and-mouth disease virus were synthesized by classic methods of peptide chemistry with isobutyl chloroformate as a coupling reagent. After purification by HPLG and amino acid analysis, the free peptides H-Gly-Lys-Tyr-Ser-Ala-Gly-Gly-Leu-Gly-Arg-Arg-Gly-OH and H-Leu-Ala-Ala-Arg-Val-Ala-Lys-Gln-Leu-Pro-OH were conjugated with BSA by means of N,N-dicyclohexylcarbodiimide. The conjugates were used, with complete Freund adjuvant, for immunization on guinea pigs.

[Synthesis of a 17-member peptide (143-159)--the VP(1) protein fragment of A(12) foot-and-mouth disease virus. II. Condensation of fragments].

A 17-membered peptide corresponding to the amino acid sequence of (143-159) site of protein VP1 of A12 foot-and-mouth disease virus has been obtained by mixed anhydride method condensations of the earlier synthesized fragments. A norleucine residue has been attached, as a label, to the ends of peptides obtained. The complete deprotection was performed by hydrogenation peptides' hydrochlorides and the products were purified by HPLC.

[Various approaches to designing the functionally active determinants as illustrated by the influenza virus A(H3N2) hemagglutinin].

Hexapeptide Lys-Gly-Pro-Asp-Ser-Gly analogous to the immunodominant fragment 141-146 of the epitope A of the influenza virus A(H3N2) hemagglutinin is synthesized. Conjugated with thyroglobulin and hemocyanine, the hexapeptide induced formation of highly specific antibodies with heterolytic properties in CBA mice. Antihexapeptide antibodies interact not only with the homologous antigen but also with hemagglutinin and influenza virus.

[Synthesis of poly (Lys-Ser-Glu) and study of its antigenic and immunogenic properties].

We have synthesized oligo- and polypeptides containing lysin, serine and glutamic acid residues. Di- and tripeptides were prepared by the successive elongation of C-terminus by means of the N,N'-dicyclohexylcarbodiimide or mixed anhydride methods. The oligopeptides were obtained by block condensation of pentafluorophenyl esters of tripeptides, and polypeptides by polycondensation of dipeptide 2,4,5-trichlorophenyl esters.

[Synthesis and catalytic activity of polypeptides of regular structure containing polyfunctional amino acids].

Synthesis and study of catalytic properties of a series of regular polypeptide which contain residues of polyfunctional amino acids forming the active centre of esterases are described viz. (Ala-Tyr-Glu)n, (His-Ser-Glu)n, (Glu-His-Glu)n, (His-Glu)n, (Ser-His-Glu)n, His-(Tyr-Glu)n. Possibility of constructing catalytically active model polypeptides which can substitute some hydrolytic enzymes is assessed.

[Study of mitochondrial permeability for labeled cAMP].

Incubation of rat liver mitochondria with 3H-and 14C-cAMP under the conditions which are conducive to the activation of mitochondrial respiration by cAMP resulted in the penetration of cAMP into the mitochondria. Subfractionation of mitochondria was made with the use of digitonin and 0.1% Triton X-100.