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Improving the Efficiency and Safety of Aspirin by Complexation with the Natural Polysaccharide Arabinogalactan Full article

Journal Current Drug Delivery
ISSN: 1567-2018 , E-ISSN: 1875-5704
Output data Year: 2016, Volume: 13, Number: 4, Pages: 582-589 Pages count : 8 DOI: 10.2174/1567201812666150605104944
Tags Analgesic; anti-inflammatory activity; aspirin; arabinogalactan; bioavailability; complexation
Authors Khvostov Mikhail V. 1 , Tolstikova Tatjana G. 1 , Borisov Sergey A. 1 , Zhukova Natalja A. 1 , Dushkin Alexander V. 2 , Chistyachenko Yulia S. 2 , Polyakov Nikolay E. 3
Affiliations
1 (Данные Web of science) NN Vorozhtsov Inst Organ Chem, Lavrentjeva Pr,9, Novosibirsk 630090, Russia
2 (Данные Web of science) Inst Solid State Chem & Mechanochem, Kutateladze,18, Novosibirsk 630128, Russia
3 (Данные Web of science) Inst Chem Kinet & Combust, Inst Skaya,3, Novosibirsk 630090, Russia

Abstract: Background: The main undesirable side effect of the aspirin is the damage to the gastrointestinal mucosa, leading to the formation of erosions, peptic ulcers, and as a result, bleeding. To overcome this problem "host-guest" complexation with natural polysaccharide arabinogalactan could be applied. Methods: The complex with a weight ratio of ASA:AG = 1:10 was prepared by solid phase method in a rotary mill. Complex was administered orally to mice or rats at doses of 250, 500 or 1000 mg/kg. The "acetic acid induced writhing" and "hot plate" tests were used as an in vivo pain models. The anti-inflammatory activity was studied using "histamine swelling" test. Also, long-term (30 days) oral introduction of the complex to rats was performed and gastric mucosa damages were evaluated. In all experiments pure aspirin (ASA) was used as a control in appropriate doses. Results: The minimal effective analgesic dose of the complex was 250 mg/kg, equivalent to 23 mg/kg of ASA, a dose in which aspirin itself was not active. The anti-inflammatory effect was found at relatively higher doses: 500 and 1000 mg/kg (46 and 92 mg/kg of ASA respectively) for the complex and only at 100 mg/kg for the ASA. Long-term introduction of the complex at doses of 250 and 500 mg/kg was safe for gastric mucosa, while ASA at the dose of 50 mg/kg showed a strong gastric mucosal damage. Conclusion: The effective analgesic and anti-inflammatory doses of 1:10 aspirin complex with arabinogalactan are twice less compared to pure aspirin and safer for the gastrointestinal mucosa.
Cite: Khvostov M.V. , Tolstikova T.G. , Borisov S.A. , Zhukova N.A. , Dushkin A.V. , Chistyachenko Y.S. , Polyakov N.E.
Improving the Efficiency and Safety of Aspirin by Complexation with the Natural Polysaccharide Arabinogalactan
Current Drug Delivery. 2016. V.13. N4. P.582-589. DOI: 10.2174/1567201812666150605104944 WOS Scopus РИНЦ
Dates:
Published print: May 21, 2016
Identifiers:
Web of science WOS:000384799900011
Scopus 2-s2.0-84973594962
Elibrary 27110891
OpenAlex W2413928644
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