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

Topical emulsions stabilized by silica nanoparticles: in vitro release and anti-inflammatory studies of flurbiprofen and diclofenac sodium

Simple and multiple emulsions have a wide range of pharmaceutical applications. Therefore, the stabilization of such emulsions is a challenge to ensure a stable formulation along the period of storage, usage and at the same time to conserve the efficacy of the incorporated medicament. Simple o/w and multiple w/o/w emulsions were prepared using castor and paraffin oils as oil phases and stabilized solely by silica nanoparticles of well-controlled surface properties. Two non-steroidal ant-inflammatory drugs, namely flurbiprofen and diclofenac sodium were incorporated in the stabilized simple and multiple emulsions, respectively. The stability of emulsions and the in vitro release of the drugs from the prepared emulsions were studied. In addition, the anti-inflammatory activity of the drugs from these liquid formulations was assessed using carageenan-induced hindpaw edema in rats. The results indicated that the prepared liquid emulsions, which stabilized with silica nanoparticles, were highly stable. The in vitro release of flurbiprofen and diclofenac sodium from these simple and multiple emulsions showed higher rates compared with those preapred from paraffin oil due to their lower viscosities. The results revealed also that the percentage of oil has a pronounced effect on the in vitro release rates of the drugs from the emulsions. Furthermore, topical flurbiprofen and diclofenac sodium emulsions exhibited a potent local anti-inflammatory activity compared with the orally adminstered drugs in the suspension form and this activity reached its peak [57-84%] 3 hrs after carrageenan injection and persisted for 5 hrs, the period of study