ArticleInflammopharmacology2026
Design, development, and optimisation of an amorphous solid dispersion-based etoricoxib bigel for targeted topical anti-inflammatory drug delivery.
Article in Inflammopharmacology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundEtoricoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, exhibits limited aqueous solubility that restricts its therapeutic performance in topical delivery systems. PURPOSE: This study aimed to develop and evaluate a novel bigel-based topical delivery system incorporating pure etoricoxib and etoricoxib-loaded amorphous solid dispersion (ASD) to enhance solubility, stability, and anti-inflammatory efficacy, with an improved onset of action. STUDY
designA Box-Behnken experimental design was employed to optimise the bigel formulation by evaluating the effects of organogelator concentration, hydrogelator concentration, and ASD percentage on viscosity, hardness, and time required for 50% drug release.
methodsBigels were prepared by blending hydrogel and oleogel phases at different ratios. The formulations were characterised for physical appearance, pH, spreadability, viscosity, and drug content. Further evaluation included rheological studies, in vitro release, and ex vivo skin permeation assessments. Dermal safety was evaluated using a skin irritation model, and anti-inflammatory activity was investigated using a carrageenan-induced paw oedema model in animals.
resultsCompatibility studies confirmed the absence of any significant interaction between etoricoxib and excipients. Carbopol 940 and stearic acid, in an 80:20 ratio, were identified as the optimised hydrogelator and organogelator, respectively. The statistical model best fitting the data was a second-order interaction (2FI) model. Increasing concentrations of hydrogelator and organogelator resulted in higher viscosity and hardness, whereas an increased proportion of ASD significantly enhanced drug release. The optimized formulation achieved ~ 80% drug release within 8 h. It showed enhanced etoricoxib permeation, with Jss (14.816 µg/cm
conclusionThe developed bigel formulation exhibited favourable physicochemical and biopharmaceutical properties, indicating strong potential as an effective topical delivery system for the management of pain and inflammation.
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