Characterization and effect of nanocomplexed fluoride solutions on the inhibition of enamel demineralization created by a multispecies cariogenic biofilm model.

OBJECTIVES: The aim of this study was to assess the in vitro caries preventive effect of nanocomplexed solutions of hydroxypropyl-ß-cyclodextrin and γ-cyclodextrin associated with titanium tetrafluoride (TiF4) after different complexation times (12 or 72 h). MATERIALS AND METHODS: Enamel blocks were randomly distributed in 9 groups (n = 11): negative control, hydroxypropyl-ß-cyclodextrin, γ-cyclodextrin, TiF4, hydroxypropyl-ß-cyclodextrin:TiF4 12 h, hydroxypropyl-ß-cyclodextrin:TiF4 72 h, γ-cyclodextrin:TiF4 12 h, γ-cyclodextrin:TiF4 72 h, and NaF (positive control). The solutions were applied for 1 min and the blocks were exposed to a biofilm model. Nanocompounds were characterized by differential scanning calorimetry and X-ray powder diffraction. The percentage of surface microhardness loss (%SML), mineral density changes (ΔZ), lesion depth, surface morphology (scanning electron microscopy-SEM), and chemical characterization (energy-dispersive spectroscopy-EDS) were assessed. RESULTS: No oxidation was observed, and the formation of the nanocomplexes was evidenced by changes in the melting point compared to pure cyclodextrins and the loss of crystallinity of the materials. Hydroxypropyl-ß-cyclodextrin:TiF4 72 h resulted in lower %SML than negative control, hydroxypropyl-ß-cyclodextrin, γ-cyclodextrin, and TiF4 (p < 0.05). NaF differed from all groups (p < 0.05), except for hydroxypropyl-ß-cyclodextrin:TiF4 72 h (p = 0.83). ΔZ of hydroxypropyl-ß-cyclodextrin:TiF4 72 h was higher than negative control, hydroxypropyl-ß-cyclodextrin, γ-cyclodextrin, γ-cyclodextrin:TiF4 1 2 h, γ-cyclodextrin:TiF4 72 h, and NaF (p < 0.05) and similar to TiF4 and hydroxypropyl-ß-cyclodextrin:TiF4 12 h (p > 0.05). SEM/EDS detected Ti in the blocks subjected to TiF4-products. CONCLUSION: The hydroxypropyl-ß-cyclodextrin:TiF4 72 h solution showed caries preventive effect on the surface and subsurface of the enamel. CLINICAL RELEVANCE: A hydroxypropyl-ß-cyclodextrin nanosystem, in association with TiF4 after 72 h of complexation, may be a promising agent for the prevention of enamel demineralization.

Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies.

BACKGROUND: Dapsone is described as being active against Mycobacterium leprae, hence its role in the treatment of leprosy and related pathologies. Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance. Nanoemulsions are pharmaceutical delivery systems derived from micellar solutions with a good capacity for improving absorption. The aim of this work was to develop and compare the permeability of a series of dapsone nanoemulsions in Caco-2 cell culture against that of effective permeability in the human body simulated using Gastroplus™ software. METHODS AND RESULTS: The release profiles of the dapsone nanoemulsions using different combinations of surfactants and cosolvent showed a higher dissolution rate in simulated gastric and enteric fluid than did the dispersed dapsone powder. The drug release kinetics were consistent with a Higuchi model. CONCLUSION: This comparison of dapsone permeability in Caco-2 cells with effective permeability in the human body simulated by Gastroplus showed a good correlation and indicates potential improvement in the biodisponibility of dapsone using this new system.