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 antiinflammatory 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.
Keywords: Analgesic, anti-inflammatory activity, aspirin, arabinogalactan, bioavailability, complexation.
Current Drug Delivery
Title:Improving the Efficiency and Safety of Aspirin by Complexation with the Natural Polysaccharide Arabinogalactan
Volume: 13 Issue: 4
Author(s): Mikhail V. Khvostov, Tatjana G. Tolstikova, Sergey A. Borisov, Natalja A. Zhukova, Alexander V. Dushkin, Yulia S. Chistyachenko and Nikolay E. Polyakov
Affiliation:
Keywords: Analgesic, anti-inflammatory activity, aspirin, arabinogalactan, bioavailability, complexation.
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 antiinflammatory 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.
Export Options
About this article
Cite this article as:
V. Khvostov Mikhail, G. Tolstikova Tatjana, A. Borisov Sergey, A. Zhukova Natalja, V. Dushkin Alexander, S. Chistyachenko Yulia and E. Polyakov Nikolay, Improving the Efficiency and Safety of Aspirin by Complexation with the Natural Polysaccharide Arabinogalactan, Current Drug Delivery 2016; 13 (4) . https://dx.doi.org/10.2174/1567201812666150605104944
DOI https://dx.doi.org/10.2174/1567201812666150605104944 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Transcranial Doppler Ultrasonography: Current Status
Current Medical Imaging Opportunities for Pharmacotherapy at the Intersection of Metabolic Syndrome and Hemostasis
Current Pharmaceutical Biotechnology Nitric Oxide and Dietary Factors: Part I Nitric Oxide Synthesis and Action
Vascular Disease Prevention (Discontinued) Assessment of Endothelial Function by Positron Emission Tomography
Current Cardiology Reviews Current Evidence and Future Perspectives on Anti-platelet and Statin Pharmacotherapy for Patients with Symptomatic Peripheral Arterial Disease
Current Vascular Pharmacology Endothelial Dysfunction and Platelet Hyperaggregation in Type 2 Diabetes Mellitus: The Era of Novel Anti-diabetic Agents
Current Medicinal Chemistry Microvascular Theory of Exercise-Induced Bronchoconstriction in Asthma: Potential Implication of Vascular Endothelial Growth Factor
Inflammation & Allergy - Drug Targets (Discontinued) Diverse Functions and Mechanisms of Pericytes in Ischemic Stroke
Current Neuropharmacology Anesthetic Considerations for Electroconvulsive Therapy-Especially Hemodynamic and Respiratory Management
Current Psychiatry Reviews Spreading Depolarization Waves in Neurological Diseases: A Short Review about its Pathophysiology and Clinical Relevance
Current Neuropharmacology Anti-VEGF Treatment in Corneal Diseases
Current Drug Targets The Janus Face of Adenosine: Antiarrhythmic and Proarrhythmic Actions
Current Pharmaceutical Design Tear Film, Conjunctival and Corneal Modifications Induced by Glaucoma Treatment
Current Medicinal Chemistry Vasomotor Effects of Iodinated Contrast Media: Just Side Effects?
Current Vascular Pharmacology Necrotizing Enterocolitis: Clinical Features, Histopathological Characteristics, and Genetic Associations
Current Pediatric Reviews Acute Respiratory Failure in Obstetric Patients
Current Women`s Health Reviews Nailfold Capillaroscopy – Its Role in Diagnosis and Differential Diagnosis of Microvascular Damage in Systemic Sclerosis
Current Rheumatology Reviews Cardiovascular Complications in Inflammatory Bowel Disease
Current Drug Targets Effect of Androgenic and Antiandrogenic Acting Compounds in Macrophage Accumulation and Cell Replication in the Aorta of Oophorectomized Hypercholesterolemic Rabbits
Vascular Disease Prevention (Discontinued) Inflammation, Endothelial Dysfunction and Arterial Stiffness as Therapeutic Targets in Cardiovascular Medicine
Current Pharmaceutical Design