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Abstract
Context: Celecoxib (CXB, 0.2 g)-loaded anionic and cationic nanosized emulsions were prepared by a well-established combined emulsification method.
Objectives: To investigate the effect of non–phospholipid-based cationic and phospholipid-based anionic emulsions on skin retention and anti-inflammatory activity of CXB.
Methods: Using Keshary-Chien diffusion cells with cellulose acetate membrane or excised rat skin, in vitro release and skin retention of CXB from solution and emulsions were studied. The anti-inflammatory activity was evaluated by the carrageenan-induced hind paw edema method in Wistar rats.
Results: The amount of drug released through artificial membrane has decreased from 122.00 ± 0.70 μg/cm2 for the CXB solution to 55.80 ± 0.70 μg/cm2 for anionic emulsion, and then further decreased to 24.79 ± 0.90 μg/cm2 for cationic emulsion. The JSS value obtained with solution, anionic, and cationic emulsions were 6825.79 ± 920.86, 2513.15 ± 382.71, and 1925.67 ± 147.42, respectively. Cationic emulsion showed a significantly higher level (P ≤ 0.05) of drug accumulation in full-thickness rat skin than anionic emulsion, and a substantially lesser percentage inhibition of edema values compared with both solution and anionic emulsion.
Discussion and conclusion: Sustained drug release together with increased skin accumulation and simultaneously decreased skin permeation as observed with cationic emulsion should substantiate its suitability as a topical delivery vehicle for CXB.
Acknowledgments
The encouragement and support given by the management of International Medical University, Malaysia, to complete the manuscript is acknowledged.
Declaration of interest
The authors report no conflicts of interest to disclose.