Isfahan University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
Effectiveness of Budesonide-Succinate-Dextran Conjugate As a Novel Prodrug of Budesonide Against Acetic Acid-Induced Colitis in Rats Publisher Pubmed



Varshosaz J1 ; Emami J1 ; Fassihi A2 ; Tavakoli N1 ; Minaiyan M3 ; Ahmadi F1 ; Mahzouni P4 ; Dorkoosh F5
Authors
Show Affiliations
Authors Affiliations
  1. 1. Department of Pharmaceutics, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  3. 3. Department of Pharmacology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  4. 4. Department of Pathology, Faculty of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran
  5. 5. Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: International Journal of Colorectal Disease Published:2010


Abstract

Background: Anti-inflammatory drugs with high potency and low systemic adverse effects, such as budesonide, are drugs of choice for the treatment of ulcerative colitis (UC). Budesonide controlled-release formulations are now being used to induce and maintain clinical remission of Crohn's disease. Budesonide-dextran conjugates were synthesized as novel prodrugs of budesonide for oral controlled delivery of the major part of the drug to the colon without needing to coat the pellets of the drug. The aim of this study was to evaluate the in vivo efficacy of this conjugate against acetic acid-induced colitis in rats. Materials and methods: Experimental UC was induced by rectal instillation of 4% solution of acetic acid to rats. After induction of colitis, rats were treated with vehicle (dextran solution), mesalasine (120 mg/kg), budesonide suspension (300 μg/kg) and BSD-70 (equivalent to 300 μg/kg of budesonide), prednisolon (4 mg/kg), hydrocortisone acetate enema (20 mg/kg), and 5-ASA enema (Asacol®) (400 mg/kg) for 5 days and then colon macroscopic and microscopic sections were examined for inflammatory response. Results: Vehicle-treated rats presented bloody diarrhoea and gross lesions. The effective formulations for attenuating the damage were BSD-70, oral prednisolon and hydrocortisone acetate enema. Rats treated with BSD-70 showed huge improvement in macroscopic and histological scores of colitis compared to the negative control group and mesalasine and budesonide suspension. Conclusion: Data indicated that budesonide-dextran conjugate is effective in improving signs of inflammation in experimental model of colitis through selective delivery of the drug to the inflamed area. © 2010 Springer-Verlag.
Related Docs
View other Related Docs
1. Preparation and in Vitro/In Vivo Evaluation of Dextran Matrix Tablets of Budesonide in Experimental Ulcerative Colitis in Rats, Drug Delivery (2011)
2. Preparation of Budesonide-Dextran Conjugates Using Glutarate Spacer As a Colon-Targeted Drug Delivery System: In Vitro/In Vivo Evaluation in Induced Ulcerative Colitis, Journal of Drug Targeting (2011)
3. Colon Delivery of Budesonide Using Solid Dispersion in Dextran for the Treatment and Secondary Prevention of Ulcerative Colitis in Rat, International Journal of Preventive Medicine (2010)
4. Microencapsulation of Budesonide With Dextran by Spray Drying Technique for Colon-Targeted Delivery: An in Vitro/In Vivo Evaluation in Induced Colitis in Rat, Journal of Microencapsulation (2011)
5. Pectin Film Coated Pellets for Colon-Targeted Delivery of Budesonide: In-Vitro/In-Vivo Evaluation in Induced Ulcerative Colitis in Rat, Iranian Journal of Pharmaceutical Research (2012)
6. Development of Novel Budesonide Pellets Based on Codes™ Technology: In Vitro/In Vivo Evaluation in Induced Colitis in Rats, DARU, Journal of Pharmaceutical Sciences (2011)
7. Anti-Inflammatory Effects of Ketotifen in Acetic Acid-Induced Ulcerative Colitis in Rats, Journal of Isfahan Medical School (2013)
8. Effect of Matricaria Aurea (Loefl.) Shultz-Bip. Hydroalcoholic Extract on Acetic Acid-Induced Acute Colitis in Rats, Iranian Journal of Basic Medical Sciences (2011)
Experts (# of related papers)
View all Related Experts
Mohsen Minaiyan (45)
Parvin Mahzouni (25)
Other Related Docs
9. Salvia Officinalis Leaf Extracts Protect Against Acute Colitis in Rats, Research in Pharmaceutical Sciences (2022)
10. Anti-Inflammatory Effect of Myrtus Communis Hydroalcoholic Extract and Essential Oil on Acetic Acid-Induced Colitis in Rats, Journal of Reports in Pharmaceutical Sciences (2019)
11. Protective Effect of Ocimum Basilicum Essential Oil Against Acetic Acid–Induced Colitis in Rats, Journal of Evidence-Based Complementary and Alternative Medicine (2016)
12. Validation and Optimization of Experimental Colitis Induction in Rats Using 2, 4, 6-Trinitrobenzene Sulfonic Acid, Research in Pharmaceutical Sciences (2012)
13. Comparative Study of Berberis Vulgaris Fruit Extract and Berberine Chloride Effects on Acetic Acid-Induced Colitis in Rats, Iranian Journal of Pharmaceutical Research (2011)
14. Effects of Carum Carvi L. (Caraway) Extract and Essential Oil on Tnbs-Induced Colitis in Rats, Research in Pharmaceutical Sciences (2013)
15. Preventive Therapy of Experimental Colitis With Selected Iron Chelators and Anti-Oxidants, International Journal of Preventive Medicine (2012)
16. Involvement of 5Ht3 Receptors in Anti-Inflammatory Effects of Tropisetron on Experimental Tnbs-Induced Colitis in Rat, BioImpacts (2013)
17. Anti-Inflammatory Effect of Volatile Oil and Hydroalcoholic Extract of Rosa Damascena Mill. on Acetic Acid-Induced Colitis in Rats, Research in Pharmaceutical Sciences (2015)
18. Development and Validation of a Rapid Hplc Method for Simultaneous Analysis of Budesonide and Its Novel Synthesized Hemiesters in Colon Specific Formulations, Research in Pharmaceutical Sciences (2011)
19. Effects of Extract and Essential Oil of Rosmarinus Officinalis L. on Tnbs-Induced Colitis in Rats, Research in Pharmaceutical Sciences (2011)
20. Protective Effects of Walnut Extract Against Oxidative Damage in Acetic Acid-Induced Experimental Colitis Rats, Physiology and Pharmacology (Iran) (2019)
21. Protective Effect of Apium Graveolens L. (Celery) Seeds Extracts and Luteolin on Acetic Acid-Induced Colitis in Rats, International Journal of Preventive Medicine (2021)
22. Evaluation of Central and Peripheral Effects of Doxepin on Acetic Acid-Induced Colitis in Rat and the Involved Mechanisms, EXCLI Journal (2017)
23. Evaluation of Anti-Ulcerative Effect of Eryngium Billardieri Extracts on Experimental Colitis in Rats, Physiology and Pharmacology (Iran) (2024)
24. Anti-Inflammatory Effect of Curcuma Longa on Ulcerative Colitis Caused Via Acoh in Rats, Journal of Medicinal and Chemical Sciences (2023)
25. Evaluating the Role of Biochanin a in Acetic Acid-Induced Colitis in Rats: Involvement of Nitric Oxide Pathway, Research Journal of Pharmacognosy (2024)
26. Ameliorative Effect of Galantamine on Acetic Acid-Induced Colitis in Rats, Research in Pharmaceutical Sciences (2019)
27. Anti-Inflammatory Effect of Prunus Armeniaca L. (Apricot) Extracts Ameliorates Tnbs-Induced Ulcerative Colitis in Rats, Research in Pharmaceutical Sciences (2014)
28. Anti-Inflammatory Effect of Apigenin and Hydroalcoholic Extract of Dracocephalum Kotschyi on Acetic Acid-Induced Colitis in Rats, Research in Pharmaceutical Sciences (2017)
29. Anti-Inflammatory and Analgesic Properties of Heracleum Persicum Essential Oil and Hydroalcoholic Extract in Animal Models, Journal of Ethnopharmacology (2009)
30. Investigating the Impact of Selected B Vitamins (B1, B2, B6, and B12) on Acute Colitis Induced Experimentally in Rats, International Journal of Preventive Medicine (2024)
31. Evaluation of Anti-Colitic Effect of Fluvoxamine Against Acetic Acid-Induced Colitis in Normal and Reserpinized Depressed Rats, European Journal of Pharmacology (2015)
32. Preparing Simvastatin Nanoparticles by a Combination of Ph-Sensitive and Timed-Release Approaches for the Potential Treatment of Ulcerative Colitis, Journal of Biomaterials Applications (2022)
33. Analgesic and Anti-Inflammatory Activities of Bupropion in Animal Models, Research in Pharmaceutical Sciences (2014)
34. Effect of a Selection of Skin Penetration Enhancers on Topical Anti-Inflammatory Effect of Boswellic Acids in Carrageenan-Induced Paw Edema in Rats, Advanced Biomedical Research (2021)
35. Anti-Inflammatory Effect of Ondansetron Through 5-Ht 3 Receptors on Tnbs-Induced Colitis in Rat, EXCLI Journal (2012)
36. Evaluating Anti-Inflammatory Effect of Hydroalcoholic Extracts of Citrus Medica L. Pulp and Peel on Rat Model of Acute Colitis, Research Journal of Pharmacognosy (2023)
37. Protective Effect of Ginger Volatile Oil Against Acetic Acid-Induced Colitis in Rats: A Light Microscopic Evaluation, Journal of integrative medicine (2014)
38. Protective Effect of Two Extracts of Cydonia Oblonga Miller (Quince) Fruits on Gastric Ulcer Induced by Indomethacin in Rats, International Journal of Preventive Medicine (2017)
39. A Systematic Review of the Clinical Use of Curcumin for the Management of Gastrointestinal Diseases, Advances in Experimental Medicine and Biology (2021)
40. Colon-Specific Delivery of Mesalazine Chitosan Microspheres, Journal of Microencapsulation (2006)
41. Effect of Venlafaxine on Experimental Colitis in Normal and Reserpinised Depressed Rats, Research in Pharmaceutical Sciences (2015)
42. Antioxidant Effects of Methanol Extract of Dracocephalum Kotschyi in Acetic Acid Induced Rat Colitis Model, Journal of Advances in Medical and Biomedical Research (2022)
43. Effect of Salbutamol Against the Experimental Acute Colitis in Rat Model, Comparative Clinical Pathology (2017)
44. Protective Effect of Dizocilpine (Mk-801) on Tnbs-Induced Experimental Colitis in Mice, Iranian Journal of Pharmaceutical Research (2019)
45. Anti-Inflammatory Effect of Pycnocycla Spinosa Extract and Its Component Isoacetovanillone on Acetic Acid Induced Colitis in Rats, Research in Pharmaceutical Sciences (2015)
46. Anti-Inflammatory Effect of Amitriptyline on Ulcerative Colitis in Normal and Reserpine-Induced Depressed Rats, Iranian Journal of Pharmaceutical Research (2016)
47. Colon Specific Delivery of Budesonide Based on Triple Coated Pellets: In Vitro/In Vivo Evaluation, Acta Pharmaceutica (2012)
48. Protective Effect of Nanoparticles of Oleoresin of Pistacia Atlantica Var. Mutica Against Acetic Acid-Induced Ulcerative Colitis in Rats, Traditional and Integrative Medicine (2022)
49. Eudragit Nanoparticles Loaded With Silybin: A Detailed Study of Preparation, Freeze-Drying Condition and in Vitro/In Vivo Evaluation, Journal of Microencapsulation (2015)
50. The Effect of Memantine on Trinitrobenzene Sulfonic Acid-Induced Ulcerative Colitis in Mice, European Journal of Pharmacology (2016)