Formulation, Characterization, and Antifungal Efficacy of Ketoconazole Emulgel for Topical Delivery
摘要
The study aimed to formulate, characterize, and evaluate ketoconazole-loaded emulgel formulations for topical delivery with enhanced antifungal efficacy and sustained release against Candida albicans.
MethodsEight ketoconazole emulgel formulations (F1–F8) were prepared using Carbopol 934 and 940. The formulations were evaluated for appearance, homogeneity, consistency, pH, spreadability, extrudability, rheological behavior, drug content, globule size, and morphology. In vitro drug release, ex vivo permeation, antifungal activity against Candida albicans, stability studies, in vivo skin irritation, and fluorescence microscopy for skin penetration were also performed.
ResultsAll formulations showed acceptable appearance, homogeneity, and skin-compatible pH (5.3–5.8). F7 demonstrated the highest spreadability, while F1 and F3 showed superior extrudability. Drug content ranged from 73.5% to 83.31%. The optimized emulgel exhibited a globule size of 666.0 nm with a polydispersity index of 0.962, and TEM confirmed spherical, well-dispersed globules. In vitro release studies revealed sustained drug release, with F1 (93.8%) and F3 (76.2%) outperforming the marketed formulation over 24 h. Antifungal studies showed that F1 and F3 exhibited significantly higher activity against Candida albicans compared to the marketed product. Stability studies confirmed that F1 and F3 remained stable over three months. Ex vivo studies demonstrated sustained drug release from F1 and F3, while the marketed product showed immediate release. In vivo skin irritation tests indicated excellent dermal compatibility, and fluorescence microscopy confirmed enhanced skin penetration of the emulgel formulations.
ConclusionKetoconazole emulgels, particularly F1 and F3, offer a safe and effective topical delivery system with sustained release, enhanced antifungal activity, and improved skin penetration.