Preparation of Ethylcellulose Coated Gelatin Microspheres as a Multiparticulate Colonic Delivery System for 5-Aminosalicilic Acid

authors:

avatar Fatemeh Atyabi 1 , * , avatar Rudabeh Vahabzadeh 1 , avatar Rassoul Dinarvand 1

Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
Iranian Journal of Pharmaceutical Research: Vol.3, issue 2; 81-86
published online: November 20, 2010
article type: Research Article
received: August 01, 2003
accepted: July 01, 2004
DOI: https://doi.org/10.22037/ijpr.2010.580

how to cite: Atyabi F, Vahabzadeh R, Dinarvand R. Preparation of Ethylcellulose Coated Gelatin Microspheres as a Multiparticulate Colonic Delivery System for 5-Aminosalicilic Acid. Iran J Pharm Res. 2004;3(2):e128186. https://doi.org/10.22037/ijpr.2010.580.

Abstract

In the long-term management of ulcerative colitis patients, repeat dosing maybe required. Since 5-ASA is largely absorbed from the upper intestine, selective delivery of drugs into the colon may be regarded as a better method of drug delivery with fewer side effects and a higher efficacy. The aim of this study was to prepare and evaluate a double coated multiparticulate system for 5-ASA delivery using gelatin and ethylcellulose as the primary and secondary polymer respectively. Gelatin microspheres containing 5-aminosalicylic acid was produced using the solvent evaporation method. Prepared gelatin microspheres were spherical, free flowing, non-aggregated and showed no degradation in the acidic medium. Entrapment efficacy of microspheres was about 50%. Results showed that drug release was fast and complete and is affected by the amount of core material entrapped. Gelatin microspheres were then coated by ethylcellulose using a coacervation phase separation technique. The idea for this approach was to prepare a delayed drug delivery system, in which, ethylcellulose protects particles for the first 6 h transit through the gastrointestinal tract. However, it was shown that this system could provide a suitable drug release pattern for colonic delivery of active agents, as 30% of the drug was released from the ethylcellulose-coated microcapsules within 6 h, while this amount was 90% of the loaded drug for gelatin microspheres under the same condition.