Evaluation of Ibuprofen/Chitosan Complexation Efficacy and Evaluation of Drug Release

Abstract

Introduction: Ibuprofen is one of the non-steroidal anti-inflammatory drugs (NSAIDs) which widely used in treatment of the pain and inflammatory disease in the market of Iran and world. The main disadvantages of this drug is gastrointestinal side effects especially in long-term administration. The drugs side effects induced by direct irritation stomach mucusa and indirect effect by systemic inhibition of prostaglandin and various methods had been used for decreasing of these unwanted effects. Aim of Study: In this study, we tried to use complexation of the drug with chitosan in order to decreasing GI side effects of the drug. Methods: Various methods including: Kneading, Co-evaporation, Co-precipitation, Co-grinding, Cross-linking with TPP, Media milling and Melting method were used for complexation of the drug and chitosan (low & medium molecular weight Chitosan). Pure drug, physical mixture and all formulation (with 1:1 ratio) were analyzed by DSC and FTIR for determination of any drug/polymer interaction during various complexation processes. In the second step, the drug release from all samples were measured in simulated gastric and intestinal fluids (SGF & SIF). Results: DSC and FTIR spectrums did not confirmed any Interaction between drug/polymer except of the samples were prepared by cross-liking method. Dissolution rate profiles of samples showed significant enhancement of dissolution rates and dissolution efficiency for all samples in compared with the pure drug and physical mixture for all samples especially by melting, co-precipitation and kneading methods in the first 1 and 2 hours. Conclusion: Althogh the complexation methods did not produced drug/ polymer complexes but, all of them significantly improved dissolution rate of the drug in SGF medium and cocsequently, decreased the direct irritation of stomach mucosa by un-dissolved drug particles.