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

被引：27

作者：

Chistyachenko, Yulia S. ^{[1
]}

Meteleva, Elizaveta S. ^{[1
]}

Pakharukova, Maria Y. ^{[2
]}

Katokhin, Aleksey V. ^{[2
]}

Khvostov, Mikhail V. ^{[6
]}

Varlamova, Anastasiya I. ^{[5
]}

Glamazdin, Igor I. ^{[5
]}

Khalikov, Salavat S. ^{[4
]}

Polyakov, Nikolay E. ^{[3
]}

Arkhipov, Ivan A. ^{[5
]}

Tolstikova, Tatyana G. ^{[6
]}

Mordvinov, Viatcheslav A. ^{[2
]}

Dushkin, Alexander V. ^{[1
]}

Lyakhov, Nikolay Z. ^{[1
]}

机构：

[1] Russian Acad Sci, Inst Solid State Chem & Mechanochem, Siberian Branch, Novosibirsk 630128, Russia

[2] Russian Acad Sci, Inst Cytol & Genet, Siberian Branch, Novosibirsk 630090, Russia

[3] Russian Acad Sci, Inst Chem Kinet & Combust, Siberian Branch, Novosibirsk 630090, Russia

[4] Russian Acad Sci, AN Nesmeyanov Organoelement Cpds Inst, Moscow, Russia

[5] KI Skryabin Sci Res Inst Helminthol, Moscow 117218, Russia

[6] Russian Acad Sci, NN Vorozhtsov Inst Organ Chem, Siberian Branch, Novosibirsk 630090, Russia

来源：

CURRENT DRUG DELIVERY | 2015年 / 12卷 / 05期

基金：

俄罗斯科学基金会;

关键词：

Albendazole; anthelmintic activity; inclusion complexes; increase of water solubility; mechanical activation; NMR-relaxation; DELIVERY; CAROTENOIDS; BINDING;

D O I：

10.2174/1567201812666150518094739

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

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 nana, 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.

引用

页码：477 / 490

页数：14

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