Adv Pharm Bull. 2021;11(2): 318-326.
doi: 10.34172/apb.2021.027
  Abstract View: 412
  PDF Download: 96

Research Article

The Effect of Thermal-Treating on Drug Release from Sustained Release Alginate-Eudragit RS Matrices

Ehsan Kaffash 1,2 ORCID logo, Mohammadreza Abbaspour 1,3, Hadi Afrasiabi Garekani 1,3, Zohreh Jahanian 1, Farinaz Saremnejad 4* ORCID logo, Abbas Akhgari 1,3* ORCID logo

1 Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
2 Student Research Committee, Mashhad University of Medical Sciences, Mashhad, Iran.
3 Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
4 Department of Food Science and Technology, Ferdowsi University of Mashhad, Mashhad, Iran.
*Corresponding Authors: Abbas Akhgari , Tel: +98 5131801327, Fax: +98 5138823251, Email: Akhgaria@mums.ac.ir


Purpose: The main objective of the present study was to develop the colonic delivery system for 5-aminosalicylic acid (5-ASA) as an anti-inflammatory drug.

Methods: Matrix pellets containing various proportions of alginate, calcium and Eudragit® RS were prepared by extrusion-spheronization technique. Thermal treatment was used to investigate the effect of the curing process on the surface morphology, mechanical and physicochemical properties and in vitro drug release profile of pellets. Based on the obtained results optimal formulations were selected to coating by the Eudragit® RS and subjected to a subsequent continuous dissolution test.

Results: Image analysis and also scanning electron microscopy results proved acceptable morphology of the pellets. The fourier transform infrared spectroscopy and differential scanning calorimetry studies ruled out any interactions between the formulation’s components. Curing process did not alter the mechanical properties of pellets. The release rate of the drug from matrices was prolonged due to the decreased porosity of cured pellets. Furthermore, selected cured pellets which coated with Eudragit® RS, prevented undesired premature drug release.

Conclusion: Formulation containing 17.5% calcium, 17.5% alginate, and a coating level of 10% demonstrated enhanced drug release so that provided resistance to acidic conditions, allowing complete drug release in alkaline pH, mimicking colonic environment. The slow and consistent drug release from this formulation could be used for treatment of a broader range of Inflammatory bowel disease (IBD) patients especially in whom colonic pH levels have been measured at lower than pH 7.0.

Keywords: Alginate, Calcium, Eudragit® RS, 5-aminosalicylic acid, Pellet, Curing
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Submitted: 04 Feb 2020
Revision: 24 Mar 2020
Accepted: 19 Apr 2020
ePublished: 19 Apr 2020
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