Abstract

EFFECT OF CERTAIN POLYMERS ON THE ULCEROGENIC ACTIVITY OF A NON-STEROIDAL ANTI-INFLAMMATORY DRUG

Esmat Zien El-Deen*, Mamdouh Ghorab, Shadeed Gad, Heba Yassin

Abstract

Diclofenac sodium (DS) is a potent non-steroidal drug with potent analgesic and anti-inflammatory activity. DS is well known to cause gastroduodenal mucosal lesions as an adverse effect. Recently, the serious problem of NSAID-induced small intestinal damage has become a topic of great interest to gastroenterologists. These attributes make diclofenac a good candidate for controlled release dosage form, so as to ensure slow release of the drug in the stomach. The present study reports on the formulation of diclofenac loaded Eudragit RS100, Eudragit RL100, Ethyl cellulose sodium alginate as well as HPMC as a controlled release drug delivery system. Solid dispersion and microencapsulation by ionotropic gelation technique were the techniques of choice in order to coat the drug so as to improve bioavailability and stability and also target a drug at specific sites. The ratio of (1:3) drug to polymer from all polymers used from solid dispersions systems and the best ratio from microbeads were selected to conduct further in vivo evaluation, since it was the best ratio which achieved significant reduction in the release of diclofenac at acidic pH of the stomach and maximal release at alkaline pH of the intestine. The obtained In vivo results indicate that microencapsulation technique was able to protect the stomach from ulcerogenic effect of diclofenac compared to solid dispersion technique.

Keywords: Diclofenac sodium, Solid dispersion, microbeads, ulcerogenic effect of diclofenac, controlled release system.