ENHANCEMENT OF DISSOLUTION AND ANALGESIC ACTIVITY OF CELECOXIB USING TERNARY SYSTEM

Abstract

The purpose of the present study is to investigate the drugloaded solid dispersion system consisting of a drug, a carrier and asurfactant. Solid dispersions of a water insoluble drug celecoxib(CX) with PVP 40000, namely binary solid dispersion systems, wasprepared at different ratios of drug to carrier [(1:1), (1:3), and(1:5)]. Polysorbate 80, a nonionic surfactant, was incorporatedinto the binary solid dispersion systems as a third component toobtain the ternary solid dispersion system. The solubilizing andabsorption enhancement properties of ternary solid dispersionsystem have been investigated. The prepared solid dispersionsystems (binary or ternary), at various drug- polymer ratios bymixing or co-precipitation, were characterized by differentialscanning calorimetery and X- ray diffractometry. The results show a remarkably improved dissolution of the drug from the ternarysolid dispersion systems when compared to the binary soliddispersion systems. The therapeutic activity of the ternary systemwas evaluated using acetic acid- induced writhing method. In-vivoexperiments in mice demonstrated that the investigated ternarysystem (drug, polymer and surfactant) shows a greater reduction ofacetic acid- induced writhing in comparison with pure drug.Moreover, the ternary system of (CX) demonstrated antiwrithingpotency 1.45 times higher than the respective binary system. Thus,the solubilizing power, the dissolution effect, and the analgesiceffect were enhanced upon the addition of the investigatedsurfactant to the binary system of celecoxib and the polymer.