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
-
Vasomotor Effects of Iodinated Contrast Media: Just Side Effects?
Current Vascular Pharmacology Recurrent Gastrointestinal Bleeding in a Patient with Eisenmenger Syndrome Using Bosentan
Current Drug Safety Clinical and Pre-clinical Applications of the Transcendental Meditation Program® in the Prevention and Treatment of Essential Hypertension and Cardiovascular Disease in Youth and Adults
Current Hypertension Reviews An Overview on Application of Natural Substances Incorporated with Electrospun Nanofibrous Scaffolds to Development of Innovative Wound Dressings
Mini-Reviews in Medicinal Chemistry Vascular Pathology from Smoking: Look at the Microcirculation!
Current Vascular Pharmacology Nitric Oxide-Dependent Neovascularization Role in the Lower Extremity Disease
Current Pharmaceutical Design The Role of Asymmetric Dimethylarginine (ADMA) in Endothelial Dysfunction and Cardiovascular Disease
Current Cardiology Reviews Nanostructures for Drug Delivery to the Brain
Current Medicinal Chemistry Musculoskeletal US: Taking the Management of Psoriatic Arthritis to a New Horizon
Current Rheumatology Reviews Vascular Endothelium: Functioning in Norm, Changes in Atherosclerosis and Current Dietary Approaches to Improve Endothelial Function
Mini-Reviews in Medicinal Chemistry Topical Bimatoprost Insert for Primary Open-Angle Glaucoma and Ocular Hypertension Treatment - A Phase II Controlled Study
Current Drug Delivery Exploring the use of Estrogen & Progesterone Replacement Therapy in Subarachnoid Hemorrhage
Current Drug Safety Pregnancy and Sleep Apnea
Current Respiratory Medicine Reviews Modeling of LIM-Kinase 2 Inhibitory Activity of Pyrrolopyrimidine Analogues: Useful in Treatment of Ocular Hypertension and Glaucoma
Medicinal Chemistry ATP-Sensitive Potassium Channels
Current Pharmaceutical Design Capsule Endoscopy in Crohn’s Disease
Current Drug Targets Intracoronary Injection of Drugs to Treat No – Reflow Phenomenon and Microcirculatory Dysfunction
Cardiovascular & Hematological Agents in Medicinal Chemistry Endothelial (Dys)Function in Lone Atrial Fibrillation
Current Pharmaceutical Design Statins and Portal Hypertension: A New Pharmacological Challenge
Current Vascular Pharmacology On the Biomaterials for Nanostructured Ocular Therapeutics
Current Organic Chemistry