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.
Keywords: Albendazole, anthelmintic activity, inclusion complexes, increase of water solubility, mechanical activation, NMRrelaxation.
Current Drug Delivery
Title:A Physicochemical and Pharmacological Study of the Newly Synthesized Complex of Albendazole and the Polysaccharide Arabinogalactan from Larch Wood
Volume: 12 Issue: 5
Author(s): Yulia S. Chistyachenko, Elizaveta S. Meteleva, Maria Y. Pakharukova, Aleksey V. Katokhin, Mikhail V. Khvostov, Anastasiya I. Varlamova, Igor I. Glamazdin, Salavat S. Khalikov, Nikolay E. Polyakov, Ivan A. Arkhipov, Tatyana G. Tolstikova, Viatcheslav A. Mordvinov, Alexander V. Dushkin and Nikolay Z. Lyakhov
Affiliation:
Keywords: Albendazole, anthelmintic activity, inclusion complexes, increase of water solubility, mechanical activation, NMRrelaxation.
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.
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S. Chistyachenko Yulia, S. Meteleva Elizaveta, Y. Pakharukova Maria, V. Katokhin Aleksey, V. Khvostov Mikhail, I. Varlamova Anastasiya, I. Glamazdin Igor, S. Khalikov Salavat, E. Polyakov Nikolay, A. Arkhipov Ivan, G. Tolstikova Tatyana, A. Mordvinov Viatcheslav, V. Dushkin Alexander and Z. Lyakhov Nikolay, A Physicochemical and Pharmacological Study of the Newly Synthesized Complex of Albendazole and the Polysaccharide Arabinogalactan from Larch Wood, Current Drug Delivery 2015; 12 (5) . https://dx.doi.org/10.2174/1567201812666150518094739
DOI https://dx.doi.org/10.2174/1567201812666150518094739 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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