Background and Objectives: Dermatophytosis (topical fungal infection) is the 4th common
disease in the last decade, affecting 20-25% world’s population. Patients of AIDS, cancer, old age senescence,
diabetes, cystic fibrosis become more vulnerable to dermatophytosis. The conventional topical
dosage proves effective as prophylactic in preliminary stage. In the advanced stage, the therapeutics
interacts with healthy tissues before reaching the pathogen site, showing undesirable effects, thus resulting
in pitiable patient compliance. The youngest carbon nano-trope “Graphene” is recently used to manipulate
bioactive agents for therapeutic purposes. Here, we explore graphene via smart engineering by
virtue of high surface area and high payload for therapeutics and developed graphene–ketoconazole
nanohybrid (Gn-keto) for potent efficacy towards dermatophytes in a controlled manner.
Methods: Polymethacrylate derivative Eudragit (ERL100 and ERS 100) microspheres embedded with
keto and Gn-keto nanohybrid were formulated and characterized through FTIR, TGA, and SEM. In vitro
drug release and antifungal activity of formulated Gn-keto microspheres were assessed for controlled
release and better efficacy against selected dermatophytes.
Results: Presence of numerous pores within the surface of ERL100 microspheres advocated enhanced
solubility and diffusion at the site of action. Controlled diffusion across the dialysis membrane was observed
with ERS100 microspheres owing to the nonporous surface and poor permeability. Antifungal
activity against T. rubrum and M. canis using microdilution method focused on a preeminent activity
(99.785 % growth inhibition) of developed nanohybrid loaded microspheres as compared to 80.876% of
keto loaded microspheres for T. rubrum. The culture of M. canis was found to be less susceptible to
Conclusion: Synergistic antifungal activity was achieved by nanohybrid Gn-Keto loaded microspheres
against selected topical fungal infections suggesting a vital role of graphene towards fungi.