Aim: The aim of this study was to develop effective topical antifungal formulation containing sertaconazole nitrate.
Background: Sertaconazole nitrate, a topical antifungal, was incorporated in solid-liquid lipid nanostructures and gelled further for topical application.
Objective: The objective of this investigation was to develop a topical formulation containing sertaconazole nitrate which was incorporated in the solid-state of the matrix to prolong the release in deep skin infection and hence reduce the application frequency.
Methods: The nanostructured lipid carriers of sertaconazole nitrate were developed by high-speed homogenization followed by ultrasonication using Estosoft-GTS® (glyceryl tristearate) as a solid lipid, oleic acid as liquid lipid and Tween 80 as an emulsifier. The central composite design was used to optimize total lipid concentration and fraction of liquid lipid in the total lipid and its effect on entrapment efficiency and drug release was determined.
Results: The carrier particles had an average size of 366.3 nm; entrapment efficiency in between 50.66% to 87.36%; cumulative drug release up to 92.90% and zeta potential of 7.43 mV. Characterization by FTIR indicated no negative interaction between drug and excipients, XRD showed the disappearance of crystalline peaks of the encapsulated drug while DSC revealed complete solubilization of the drug. About 99.6% of the drug was estimated by HPLC method. The drug release from gel and cream was 25.04% and 72.97% respectively. The lipid and gel excipients did not interfere with the antifungal activity of the drug.
Conclusion: The developed nanocarriers loaded gel was stable. It prolonged the drug release (for 24 h) than marketed cream. It could be a promising concept for the topical delivery of antifungal and anti-inflammatory materials.