No abstract

Objective: Posaconazole(POS) is an antifungal drug widely used in treatment of fungal infections. However, the drug has very low oral bioavailability due to high first-pass metabolism, thereby limiting its therapeutic effectiveness. The present study is aimed to prepare nanoemulsion of posaconazole to increase its solubility and to develop posaconazole-loaded nanoemulsion based gel for single dose topical administration to sustain the release of the drug, improve patient compliance and avoid repeated administration. Method:-FTIR-study was performed to determine compatibility of drug with excipients. Pseudoternary-phase diagram was constructed to optimize the Smix ratio. Optimization of nanoemulsion was done by Box-Behnken Design. The optimized formulation was evaluated for particle-size (nm), polydispersity index (PDI), (%) drug content and in-vitro drug release. POS-nanoemulgel (FNG) was developed using carbopol-934P (1%), which was evaluated for homogeneity, pH, viscosity, spreadability, percentage-yield and in-vitro drug release. The anti-fungal activity of POS-nanoemulgel was evaluated against Candida Albicans. Results: The FTIR-study confirmed that there was no interaction between drug and excipients. The optimized selected nanoemulsion (FN1) exhibited particle size 79.19nm, PDI 0.357, drug content 95.90% and in-vitro release of 79.40% at 24 hour. The prepared nanoemulgel was homogenous, opaque with good spreadability 13.91±1.19, viscosity 3760±0.014, pH 5.6±0.06 and the zeta-potential was -29mV, indicating good stability. The drug release at 24h was 72.01%. Further, the developed nanoemulgel formulation exhibited better antifungal activity in comparison to the pure drug gel. Conclusion: Hence, it can be concluded that nanoemulgel of posaconazole can provide better antifungal activity and improve patient compliance. Keywords: Nanoemulsion, Nanoemulgel, Posaconazole, Anti-fungal, Box-Behnken Design, Pseudoternary phase diagram.