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

Abstract

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. The mechanochemically synthesized complexes were more stable in comparison with the complex produced by mixing solutions of the components. The complexes of ABZ showed anthelmintic activity at 10-fold lower doses than did free ABZ. The complexes also showed lower acute toxicity and hepatotoxicity. These results suggest that it is possible to design new drugs on the basis of the ABZ:arabinogalactan complex that are safer and more effective than albendazole.

Complex Preparations for the Protection Potato on the Basis of Tebuconazole

“…All the studied preparations applied to the tubers, both in autumn and spring, to the full germination phase compared with the control significantly reduced [10]. The same results were showed for anthelmintic drugs by creating water-soluble compositions of lipophilic drug compounds [11]. It was demonstrated an increase in the solubility and penetration ability of TBC into plant objects [12].…”

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

“…Probably, this is along with an increase in solubility, this factor can also serve to increase the anthelmintic activity of the obtained drugs. The formation of the supramolecular complex of fenbendazole with PVP occurs according to the “guest-host” scheme described earlier [39,40]. So, hydrophobic interactions of “guest-host” type could facilitate the creation of supramolecular complexes where “guest” is the molecules of fenbendazole and the polymer is a “host” acting as a medication carrier.…”

Solid Dispersions of Biologically Active Substances

“…Were obtained SD of ABZ and FBZ with polysaccharides -AG, Hydroxyethyl Starch / HES / and polymer PVP. The formation of these SD were confirmed by the above methods [32][33][34][35][36][37][38][39]. The molecular dynamics of the complexes in solution was studied using 1 H NMR.…”

“…Expanding the spectrum of benzimidazole anthelmintics [31], were selected the substances of ABZ, FBZ, TCB and their mixtures, which were modified with such polymers as PVP, polysaccharides (AG, glycyrrhizic acid /GA/ and its derivatives), auxiliary substances (silica gel, others) . The machining of the components was carried out in a metal drum with steel balls in an LE-101 roller mill (manufactured in Hungary) and the corresponding SD were obtained, which were characterized by X-ray and DSC analysis, SEM, IR-spectroscopy, and dissolution in water [32][33][34][35] .…”