Biological Activity and Pharmacokinetic Behavior of Fenbendazole Integrated into a Supramolecular Delivery System with Licorice Extract and Sodium Dioctyl Sulfosuccinate

Varlamova, A.I.; Movsesyan, S.O.; Arkhipov, I.A.; Khalikov, S.S.; Arisov, M.V.; Kochetkov, P.P.; Abramov, A.E.; Ilyin, M.M.; Lokshin, B.V.

Авторы: Varlamova A.I., Movsesyan S.O., Arkhipov I.A., Khalikov S.S., Arisov M.V., Kochetkov P.P., Abramov A.E., Ilyin M.M., Lokshin B.V.
Журнал: Biology Bulletin
Том: 47
Номер: 6
Год издания: 2020
Издательство: M A I K Nauka - Interperiodica
Местоположение издательства: Russian Federation
Первая страница: 549
Последняя страница: 558
Оригинальные версии: Биологическая активность и особенности фармакокинетики фенбендазола на основе супрамолекулярной системы адресной доставки с экстрактом солодки и диоктилсульфосукцинатом натрия
DOI: 10.1134/S1062359020060138
Аннотация: A supramolecular complex (SFBZ) of fenbendazole (FBZ) with licorice extract and sodium dioctylsulfosuccinate is prepared by mechanochemical method, and its anthelminthic activity and metabolism insheep are studied. Physicochemical studies of SFBZ confirmed its improved solubility and a decrease in theparticle size. FBZ and its metabolites are found to display enhanced absorption into the bloodstream. Theirmaximum concentration in the blood increases by a factor of 2.3–2.5, and the time required to reach this levelincreases. The efficacy of SFBZ on the laboratory model of Trichinella spiralis infection is 96.27% at a doseof 1 mg/kg a.i. (active ingredient), whereas the efficacy of the FBZ substance administered at the same doseis 13.70%. A single oral dose of 2.0 mg/kg (a.i.) of SFBZ is highly effective against nematodes in naturallyinfected sheep, as fecal analyses showed; while the FBZ substance revealed 95.97% efficacy at a dose of5.0 mg/kg. The higher activity of SFBZ is related to its increased solubility and improved absorption in theanimal body.
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