Statistical Optimization of Nano Emulsion-Based Gel of Efinaconazole for Onchomycosis

Background

The objective of this study is to create a nano emulsion-based gel, of efinaconazole, a class II (BCS) antifungal medication for onchomycosis, by increasing solubility.

Materials and Methods

Solubility studies in oils, surfactants were conducted. Medication and excipients compatibility was studied by FTIR analyses. Emulsion zone for certain emulgent, oil and water components was determined by Ternary phase diagrams. Statistical optimization by D-optimal design with oil phase (oleic acid), emulgent (Transcutol), water phase as X1, X2, X3 (respectively) dependent variables and responses drug content (R1), drug release percentage (R2) as independent variables. Physico-chemical parameters of nanoemulsion and gel were evaluated along with zeta potential for optimized formulation.

Results and Discussion

Dependent variables, drug content (R1) follows reduced quadratic model and linear model for % drug release (R2) from lack of fit summary. The optimized nanoemulsion formulation NEP-17 containing Oil (31.29 mL), emulgent (58.70 mL), water (10.00 mL) showed 82.19±0.01% of drug release after 8 hr, drug content 100.7%, 229.7nm Globule size, PDI of 0.284, Zeta-potential of -42.1 mV was formulated into carbopol gel G2. It followed anomalous transport mechanism and was stable. Antifungal studies against Candida albicans and Candida glabrata of G2 were compared with marketed Luliconazole solution 1% (LUZU).

Conclusion

The results suggest that nano emulsion gel has enhanced solubility to boost bioavailability.