Nanostructured formulations to be used as desensitizers during in-office tooth bleaching: development, pharmacological characterization, transdental permeability, and cytocompatibility
Nanogels; Dexamethasone; Codeine; Tooth Remineralization; Tooth Permeability.
Despite the effectiveness of in-office tooth bleaching with hydrogen peroxide, side effects like bleaching sensitivity and immediate mineral loss persist. This study aimed to develop nanostructured formulations to be used as desensitizers during in-office tooth bleaching, characterize their pharmacological properties, and evaluate their transdental permeability and cytocompatibility. Nanoemulsions (NEs) and nanogels (NGs) containing dexamethasone acetate (DEX), codeine (COD), and/or calcium phosphate for topical use were synthesized. NEs were prepared using the phase inversion method, varying the surfactant concentration (SC) from 1 to 5%. The most stable formulation with the lowest SC was selected for physicochemical characterization over 45 days, during which droplet size, polydispersity index (PdI), zeta potential (ZP), and pH were evaluated. Nanosystems were analyzed using Fourier-transform infrared (FTIR) spectroscopy, Transmission Electron Microscopy (TEM), and spectrophotometry. The formulations underwent hemolytic evaluations and cell tests. In vitro permeability was analyzed using a standardized device with human third molar discs. NGs were applied before and after bleaching with 35% hydrogen peroxide (three applications of 15 minutes each). Data were analyzed using two-way ANOVA followed by Tukey´s post hoc test via GraphPad Prism software (p<0.05). Characterization revealed that NE contained 100% COD and 80% DEX, with an average droplet size of approximately 170 nm, PdI > 0.3, negative PZ, and a pH close to neutral. The immediate drug release showed a content of 4%. All formulations demonstrated cell viability (p<0.0001) and hemolytic potential below 30% (p<0.0001). Therefore, the formulations exhibited suitable pharmacological properties, allowed drug permeation through dental structures, and were shown to have cytocompatibility.