Abstract
Background: Treatment of fungal infection through oral route is avoided since topical delivery has ease of application and improved patient compliance. Topical drug delivery is used for local administration of drug directly to the affected area, resulting in localization of drug.
Objective: The objective of the present study was to prepare and evaluate fluconazole (FLZ) loaded microemulsion (ME) based gel for topical delivery.
Methods: Triacetin as the oil phase, tween 80 as surfactant and ethanol as cosurfactant were screened as microemulsion components. Pseudoternary phase diagrams were constructed by titration method and various MEs was prepared and evaluated for parameters like globule size, poly dispersibilty index (PDI), viscosity, pH, and stability. Finally, optimized microemulsion (ME9) was selected to prepare various gels and evaluated for drug content, viscosity, pH and spreadability. Optimized microemulsion based hydrogel containing carbopol 934 (MBH6) was compared with marketed formulation or ex vivo permeation study using rat skin. The optimized MBH6 and marketed formulation were also evaluated for antifungal activity against fungal strain Microsporum fulvum (MTCC 16446) as well as for skin irritation studies.
Results: The studied optimized MBH6 showed a good stability over a period of 6 months. The average globule size of optimized ME9 was found 36.17 nm. The antifungal activity of MBH6 was found comparable to the marketed formulation.
Conclusion: It was concluded that the proposed microemulsion based hydrogel (MBH6) is a promising delivery vehicle for topical delivery of FLZ.
Keywords: Fluconazole, carbopol 934, microemulsion based hydrogel, topical delivery, Microsporum species.
Graphical Abstract
53
4