ENHANCEMENT OF DISSOLUTION AND ANALGESIC ACTIVITY OF CELECOXIB USING TERNARY SYSTEM

The purpose of the present study is to investigate the drug
loaded solid dispersion system consisting of a drug, a carrier and a
surfactant. Solid dispersions of a water insoluble drug celecoxib
(CX) with PVP 40000, namely binary solid dispersion systems, was
prepared at different ratios of drug to carrier [(1:1), (1:3), and
(1:5)]. Polysorbate 80, a nonionic surfactant, was incorporated
into the binary solid dispersion systems as a third component to
obtain the ternary solid dispersion system. The solubilizing and
absorption enhancement properties of ternary solid dispersion
system have been investigated. The prepared solid dispersion
systems (binary or ternary), at various drug- polymer ratios by
mixing or co-precipitation, were characterized by differential
scanning calorimetery and X- ray diffractometry. The results show a remarkably improved dissolution of the drug from the ternary
solid dispersion systems when compared to the binary solid
dispersion systems. The therapeutic activity of the ternary system
was evaluated using acetic acid- induced writhing method. In-vivo
experiments in mice demonstrated that the investigated ternary
system (drug, polymer and surfactant) shows a greater reduction of
acetic acid- induced writhing in comparison with pure drug.
Moreover, the ternary system of (CX) demonstrated antiwrithing
potency 1.45 times higher than the respective binary system. Thus,
the solubilizing power, the dissolution effect, and the analgesic
effect were enhanced upon the addition of the investigated
surfactant to the binary system of celecoxib and the polymer.