Formulation, in vitro and in vivo evaluation of celecoxib nanosponge hydrogels for topical application

BackgroundCelecoxib is an extremely lipophilic and poorly water soluble NSAID which has gastrointestinal side effects when used chronically. Solubility of celcoxib is 7.6 μg/ml and therefore the oral bioavailability of celecoxib is 40% when administered as a capsule dosage form.ObjectiveThe purpose of this current study is to improve the solubility of Celecoxib using β-cyclodextrin and NN-methylene bisacrylamide Nanosponge hydrogel formulation.MethodsNanosponges of celecoxib were prepared and characterized by differential scanning colorimetry, X-ray diffractometry, FT-IR analysis and evaluated by Zeta-potential and Polydispersity index and drug entrapment efficiency. Further, celecoxib nanosponges were dispersed in 1% carbopol 934 hydrogel and the gel was evaluated for its viscosity, pH, spreadability, in vitro diffusion. In vivo, pharmacokinetic and skin irritation studies conducted using rats.ResultsSolubility of freeze dried nanosponge particles were in the range of 230.49 ± 0.16-490.48 ± 0.88 μg/ml, which indicates 30 to 65 fold increases in the solubility compared to pure drug.ConclusionThese results confirm that nanosponge formulation is ideal for increasing the solubility and bioavailability of poorly water soluble drug like celecoxib.

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