Pharmacological activity and targeted delivery of supramolecular fenbendazole obtained by mechanochemical technology with various components

The purpose of the research is studying the influence of various components on the targeted delivery of fenbendazole and evaluation of their efficacy in mice experimentally infected with Trichinella spiralis.Materials and methods. The experiment used 80 white mice experimentally infected with T. spiralis, at a dose of 200 larvae per animal. Each group of 10 animals was administered intragastrically solid dispersion of fenbendazole (SDF) with polyvinyl pyrrolidone (PVP), arabinogalactan (AG), disodium salt of glycyrrhizinic acid (Na2 GA), sodium dioctyl sulfosuccinate (SDS), licorice extract (LE) and hydroxyethyl starch (HES) at a single dose of 2.0 mg/kg of active substance as compared with the fenbendazole substance at the same dose. The control group did not receive the drug. The anthelmintic efficacy was studied by the results of necropsy of the small intestine of mice on the second day after drugs administration. The concentration of fenbendazole and its metabolites in the small intestine was determined by high-performance liquid chromatography with tandem mass spectrometry detection.Results and discussion. SDF with PVP, AG, Na2 GA, SDS, LE and HES showed 98.0, 94.9, 96.6, 100, 86.0 and 81.0% efficacy against intestinal nematode T. spiralis at a dose of 2.0 mg/kg of AS (fenbendazole). The maximum concentration of fenbendazole and its metabolites – sulfone and sulfoxide - was determined in the small intestine wall of animals on the second day after SDF with SDS administration and amounted to 3117.8, 614.6 and 2998.6 ng/g respectively. After fenbendazole substance administration, the drug and its metabolites were found in trace quantity.

MECHANOCHEMICAL MODIFICATION OF TRICLABENDAZOLE FOR THE PRODUCTION OF AN EFFECTIVE ANTI-FASCILOID DRUG

Continuing a series of studies to increase the solubility of the known substance triclabendazole (TСB), the technology of mechanochemical modification was used with a mixture of polymers-polyvinylpyrrolidone (PVP) and arabinogalactan (AG) with the addition of the known emulsifier – sodium dioctyl sulfosuccinate (SDN). In this case, solid dispersions (SD) of TCB compositions were obtained: TCB : PVP = 1: 9, TCB : PVP : AG = 1: 4.5: 4.5 and TCB : PVP : AG : SDN = 1: 4.5: 4.5: 0.1, which are easily loose powders that form stable suspensions in water when preparing working solutions for use in animals. A significant improvement in the solubility (almost 30 times) of the obtained SDs with the addition of SDN was established, which allows us to hope for their high antifascioid activity. Drugs can also be used for use by adding to animal feed. Currently, the drug is being tested in laboratory and industrial conditions. According to preliminary data, drugs with the addition of SDN are of interest and additional studies are required for implementation in veterinary practice.

Electrochemical synthesis and characterizations of new nanocomposite electrodeposition on Co67Cr29W4 alloy substrate

In this study, galvanostatic electrodeposition techniques were employed for the achieved of new composite polymer: polypyrrole - sodium dioctyl sulfosuccinate/poly N-ethylaniline (PPY-AOT/PNEA) coatings on the Co67Cr29W4 alloy electrode surface. The PPYAOT/PNEA coating has been synthesized on the Co67Cr29W4 alloy electrode by galvanostatic deposition from aqueous solutions 0.1 M NEA, 0.1M PY, 0.01 M AOT and 0.5 M H2SO4 solution at various current densities (1mA/cm2 , 2mA/cm2 and 8mA/cm2 ) in different molar ratio. The sodium dioctyl sulfosuccinate (AOT) as a dopant ion used in electropolymerization process be able to a significant influence on the electrochemical activity of the composite polymer. The polymeric composite coatings were characterized by cyclic voltammetry (CV), electrochemical impedance spectroscopy (EIS), and scanning electron microscopy (SEM) techniques. The results denoted that the electroactive behaviors of the composite polymer mainly depend on the molar ratio of monomers, the applied density current and times of electrodeposition. It has been established that the cobalt based alloy substrate had a meaningful influence on the electrochemical activity of the polypyrrole and poly(N-ethylaniline) composite films and that as in the existence of polymeric film, anodization of these modified electrodes obtained in constitution of an oxides complex film and polymeric layers together. All of the composite films were a very promising electrode material for application in supercapacitor, corrosion protection coatings or sensor employments.

Counterion binding on coacervation of dioctyl sulfosuccinate in aqueous sodium chloride

A simple coacervate-forming system consisting of sodium dioctyl sulfosuccinate (DOSS) in aqueous NaCl solution was investigated by turbidity measurement, electromotive force measurement (EMF), dynamic light scattering (DLS), and cryogenic transmission electron microscopy (cryo-TEM) to reveal the role of counterion binding in the microstructural changes behind the evolution of the coacervate phase.

Synthesis of polyethylene glycol diacrylate nanogel using irradiation of inverse micelles technique

The purpose of the work described here was to prepare covalently crosslinked nanogel from polyethylene glycol diacrylate (PEGDA) using an inverse micelle system as a template for irradiation via electron beam. Inverse micelles were formed by addition of sodium dioctyl sulfosuccinate (AOT) in n-heptane above its critical micelle concentration. These nano sized micelles were used to trap PEGDA in its water phase. Irradiation of the PEGDA containing micelles leads to formation of many radicals and recombinations thus forming crosslinked nanogel.

Nanoporous Polymeric Periodic Structures Fabricated by Emulsion-assisted Holographic Patterning

We report a new technique of creating a nanoporous polymeric nanostructure by photo-patterning emulsions generated from a formamide (polar phase) and an acrylate-monomer (nonpolar phase). Formamide is a highly polar solvent that forms well dispersed, non-aqueous emulsion droplets within the monomer-containing nonpolar phase before holographic patterning. Photochemically initiated polymerization of the nonpolar phase (acrylate monomer) forces the formation of ordered formamide emulsions defined by the holographic interference. Evaporation of the formamide from the ordered structure yields a periodic structure with high optical reflectivity and a wide reflection bandwidth. The average size and the size distribution of formamide droplets in the photopolymer fluid must be controlled to fabricate a periodic structure with high reflectivity. Furthermore, we found that the addition of sodium dioctyl sulfosuccinate (AOT) surfactant helps to stabilize the formamide emulsion which further facilitates the formation of the ordered nanopores with uniform size.