FORMULATION DEVELOPMENT AND CHARACTERIZATION OF KETOCONAZOLE ANTIFUNGAL CREAM

Abstract

Objective: Aim of the present work was formulation development and characterization of antifungal cream formulation for topical delivery of Ketoconazole in seborrheic dermatitis. Ketoconazole is a potent antifungal, BCS class II drug showing high permeability and low solubility and can be delivered topically via skin if formulated in a cream formulation with improved physicochemical characteristics, drug release behaviour, and antifungal efficacy.

Methods: Preformulation studies including solubility, melting point, and drug–excipient compatibility studies were performed to assess the suitability of ketoconazole for formulation development. Then six batches (K1–K6) were formulated using the emulsification method and optimized by characterization of their physicochemical characteristics i.e., pH, spreadability, extrudability, rheological profile, content uniformity, and physical appearance. The optimized formulation was further compared for invitro drug release profile with marketed cream formulation and evaluated for antifungal efficacy study and stability study for one month as per ICH guidelines.

Results and Discussion: The solubility study revealed higher solubility of ketoconazole in organic solvents such as methanol and ethanol compared to aqueous media, while FT-IR analysis confirmed the absence of significant interaction between the drug and selected excipients. All the formulations batches exhibited acceptable characteristics with skin-compatible pH and good homogeneity. Among the prepared formulations, batch K4 demonstrated optimal performance with suitable viscosity, excellent spreadability and extrudability, and the highest drug content (93.50 ± 1.5%). The in-vitro drug release study using Franz diffusion cell indicated that the optimized formulation (K4) showed 97.4% drug release within 5 hours, which was comparable to the marketed ketoconazole cream. Furthermore, antifungal efficacy testing against Candida albicans demonstrated a zone of inhibition of 12 ± 0.5 mm, slightly higher than the marketed formulation (11 ± 0.5 mm). Stability studies confirmed that the optimized formulation remained stable without significant changes in physicochemical parameters during storage.

Conclusion: Overall, the developed ketoconazole cream formulation exhibited satisfactory physicochemical properties, effective drug release, significant antifungal activity, and promising stability, indicating its potential as an effective topical antifungal preparation comparable to marketed formulations.