Preparation and in vitro evaluation of controlled release granules of mesalazine for colon targeted drug delivery system

Document Type : Original Article


Department of Pharmaceutics, School of Pharmacy, Shiraz University of Medical Science, Shiraz, Iran.



Targeted drug delivery systems into the colon to cure different local diseases like ulcerative colitis, cancer, and irritable bowel diseases have gained attention. These drug delivery systems are more effective for local inflammation and have limited side effects. The purpose of the present study is to formulate a controlled-release system of mesalazine, an anti-inflammatory agent by fluidized bed coating. The formulation was prepared using hydroxyl propyl methylcellulose as sustained delivery and cellulose acetate phthalate for enteric-coated behavior. The prepared granules were evaluated for particles size, moisture content, friability, dissolution test. The granules made with wet granulation had a suitable size and free flowability with carr's index lower than 20. It was concluded that the prepared granules could be successfully formulated with the use of release retarding polymers. The formulation showed appropriate release retardation of the drug, indicating the potential of a delivery system. A further investigation like capsule preparation and microbial count examination is needed for better evaluation of the formulation.
Please cite this article as: Sanaz Mehdi-alamdarlou, Negin Mozafari, Saeid Daneshamouz, Hajar Ashrafi. Preparation and in vitro evaluation of controlled release granules of mesalazine for colon targeted drug delivery system. Trends in Pharmaceutical Sciences. 2022;8(1):37-42 .doi: 10.30476/TIPS.2021.92954.1116


1. Keerthi Brahmandam K, Kothamasu S, Makineni A, Nama S. Formulation and evaluation of sitagliptin phosphate gastro retentive tablets.
Caribb J Sci Tech. 2014;2:270-81.
2. Omar S, Aldosari B, Refai H, Gohary OA. Colon-specific drug delivery for mebeverine hydrochloride. J Drug Target. 2007 Dec;15(10):691-700. doi: 10.1080/10611860701603281. PMID: 18041637.
3. Amidon S, Brown JE, Dave VS. Colon-targeted oral drug delivery systems: design trends and approaches. AAPS PharmSciTech. 2015 Aug;16(4):731-41. doi: 10.1208/s12249-015-0350-9. Epub 2015 Jun 13. PMID: 26070545; PMCID: PMC4508299.
4. Bayan MF, Bayan RF. Recent advances in mesalamine colonic delivery systems. Future J Pharm Sci. 2020;6(1):43. doi:10.1186/s433094-2--00057-7
5. Abinusawa A, Tenjarla S. Release of 5-Aminosalicylic Acid (5-ASA) from Mesalamine Formulations at Various pH Levels. Adv Ther. 2015 May;32(5):477-84. doi: 10.1007/s12325-015-0206-4. Epub 2015 May 8. PMID: 25951927; PMCID: PMC4449368.
6. Déo SC, Andreazza IF, Possamai JC. Development of mesalazine pellets coated with methacrylic-derived polymer. Braz J Pharm Sci. 2011;47:103-9.
7. Kaur G, Grewal J, Jyoti K, Jain UK, Chandra R, Madan J. Chapter 15 - Oral controlled and sustained drug delivery systems: Concepts, advances, preclinical, and clinical status. In: Grumezescu AM, editor. Drug Targeting and Stimuli Sensitive Drug Delivery Systems: William Andrew Publishing; 2018. p. 567-626.
8. Nesbitt RU, Goodhart FW, Gordon RH. Evaluation of polyvinyl acetate phthalate as an enteric coating material. Int J Pharm. 1985;26(3):215-26.
9. Shanmugam S. Granulation techniques and technologies: recent progresses. Bioimpacts. 2015;5(1):55-63. doi: 10.15171/bi.2015.04. Epub 2015 Feb 18. PMID: 25901297; PMCID: PMC4401168.
10. Agrawal R, Naveen Y. Pharmaceutical processing–A review on wet granulation technology. Int J Pharm Front Res. 2011 Apr;1(1):65-83.
11. Suresh P, Sreedhar I, Vaidhiswaran R, Venugopal A. A comprehensive review on process and engineering aspects of pharmaceutical wet granulation. Chem Eng J. 2017;328:785-815.
12. Thapa P, Tripathi J, Jeong SH. Recent trends and future perspective of pharmaceutical wet granulation for better process understanding and product development. Powder Technol. 2019;344:864-82.
13. Basavaiah K, Rajendraprasad N, Vinay KB. Isocratic High-Performance Liquid Chromatographic Assay of Olanzapine: Method Development and Validation. ISRN Anal Chem. 2014;2014:616941.
14. Patil GD, Tambe KP, Shirsat SP, Patil A. Review on enteric coated polymers. Res J Pharma Dosage Forms and Tech. 2021;13(1):82-5. 10.5958/0975.2021.00015.x
15. Mozafari N, Azadi S, Mohammadi Samani S, Farjadian F, Azadi A. Concurrent analysis of Simvastatin and citicoline using a Reversed-phase High Performance Liquid Chromatography-Ultra Violet Method. Trends in Pharmaceutical Sciences. 2019; 5(1): 41-46. doi: 10.30476/tips.2019.81749.1006.
16. Hiremath P, Nuguru K, Agrahari V. Chapter 8 - Material Attributes and Their Impact on Wet Granulation Process Performance. In: Narang AS, Badawy SIF, editors. Handbook of Pharmaceutical Wet Granulation: Academic Press; 2019. p. 263-315.
17. Efentakis M, Naseef H, Vlachou M. Two- and three-layer tablet drug delivery systems for oral sustained release of soluble and poorly soluble drugs. Drug Dev Ind Pharm. 2010 Aug;36(8):903-16. doi: 10.3109/03639040903585119. PMID: 20196641.
18. Szumilo M, Belniak P, Swiader K, Holody E, Poleszak E. Assessment of physical properties of granules with paracetamol and caffeine. Saudi Pharm J. 2017 Sep;25(6):900-905. doi: 10.1016/j.jsps.2017.02.009. Epub 2017 Feb 16. PMID: 28951676; PMCID: PMC5605841.
19. Osamura T, Takeuchi Y, Onodera R, Kitamura M, Takahashi Y, Tahara K, Takeuchi H. Formulation design of granules prepared by wet granulation method using a multi-functional single-punch tablet press to avoid tableting failures. Asian J Pharm Sci. 2018 Mar;13(2):113-119. doi: 10.1016/j.ajps.2017.08.002. Epub 2017 Aug 10. PMID: 32104384; PMCID: PMC7032211.
20. Garbacz G, Klein S. Dissolution testing of oral modified-release dosage forms.
J Pharm Pharmacol. 2012 Jul;64(7):944-68. doi: 10.1111/j.2042-7158.2012.01477.x. Epub 2012 Feb 21. PMID: 22686342.