Microemulsion containing triamcinolone acetonide for buccal administration

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Abstract

The aim of the present work was to investigate the potential of microemulsions for the buccal administration of triamcinolone acetonide. Microemulsions were developed by the construction of pseudoternary phase diagrams, using the aqueous titration method. Among all microemulsions prepared and tested for stability, three were selected and submitted to characterization and in vitro permeation/retention experiments, using pig esophageal epithelium, an accepted model of the buccal mucosa. Furthermore, one microemulsion was added of excipients (stearylamine, CTAB and chitosan) able to alter the charge of droplets.

The results obtained show that the permeation of triamcinolone acetonide across pig esophageal epithelium was not influenced by the droplet size nor by the composition, but only by the presence of chitosan, polysaccharide able to increase the transport across mono and stratified epithelia. The determination of the permeation parameters allowed us to show that chitosan acts on the diffusion parameter across the tissue and not on the partitioning parameter; for the same reason the tissue retention of triamcinolone acetonide was not modified. Triamcinolone flux (2.6 μg cm−2 h−1) was too low to make systemic administration feasible (dose required 2.5 to 60 mg/day).

The amount of triamcinolone acetonide recovered in the mucosa after only 10 min. of microemulsion application was much higher than after overnight application of the commercial paste Omicilon® A. This suggests that triamcinolone acetonide microemulsions can be an interesting alternative to the commercial formulation to treat diseases of the buccal mucosa. Owing to the fast uptake by the tissue, the formulation can be used as a mouthwash.

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