Abstract

DEVELOPMENT AND IN VITRO EVALUATION OF POLYSACCHARIDE-BASED SYSTEM FOR INTESTINAL DELIVERY OF AZATHIOPRINE FOR TREATMENT OF GASTRODUODENAL CROHN’S DISEASE, JEJUNOILEITIS AND ILEITIS

Abdelrahman M. Helmy and Elsayed A. Ibrahim*

ABSTRACT

Azathioprine is immunosuppressant drug used effectively for treatment of gastroduodenal Crohn’s disease, jejunoileitis and ileitis. The systemic administration of azathioprine is characterized by its slow onset of action and causing serious adverse effects. The objective of the current work was to develop and evaluate azathioprine-loaded pectin beads for intestinal release of azathioprine (i.e. the inflammatory disease site) to overcome the characteristic drawbacks of the systemic administration of azathioprine. Two different preparation techniques were followed to develop azathioprine-loaded pectin beads by ionotropic gelation. Several characterizations were carried out for the developed beads (e.g. size, morphological features, yield, drug loading capacity, drug entrapment efficiency and in vitro release) to select the better preparation technique, and further optimization studies were performed. Azathioprine-loaded pectin beads were successfully developed as spherical beads of 1.62 ± 0.04 mm diameter and high entrapment efficiency (c.a. 94%). The in vitro release profiles of the developed azathioprine-loaded pectin beads showed that most of the drug amounts released at intestinal simulating medium. The azathioprine-loaded pectin beads developed in the current study might have a promising potential for treatment of gastroduodenal Crohn’s disease, jejunoileitis and ileitis effectively, more effectively and more safely than the systemic administration of azathioprine.

Keywords: azathioprine, intestinal delivery, ileitis, jejunoileitis, pectin.