<p>Griseofulvin, a common antifungal, suffers from poor solubility and skin penetration, limiting its topical efficacy. The main purpose of the study is to develop and characterize a griseofulvin-loaded transfersomal gel to enhance topical delivery and sustain antifungal activity. The transfersomes were prepared by thin-film hydration with varying ratios of lecithin and Tween 80 and evaluated for vesicle size, morphology, and entrapment efficiency (EE). The optimized formulation (GRF7) had the highest EE (98.02 ± 0.55%) and the smallest nanosized spherical vesicles (167.32 ± 0.51&#xa0;nm), as confirmed by scanning electron microscopy (SEM). The GRF7 transfersomes were combined with a Carbopol 934 gel basis and tested for pH, homogeneity, spreadability, drug content, viscosity, in vitro release, kinetic release, and stability. The gel’s physicochemical parameters were acceptable, with a pH of 6.78 ± 0.42, viscosity of 31,700 cps, and homogeneous drug content (97.98 ± 0.55%). In vitro diffusion experiments indicated sustained release (90.2% from the improved formulation, GRF-7) for 18&#xa0;h. The release kinetics were consistent with the Korsmeyer-Peppas model (R²=0.996), suggesting a super case-II transport mechanism suitable for sustained-release topical systems. Over three months of short-term stability tests, there was no significant variation in pH, drug content, or release behavior. Overall, the griseofulvin-loaded transferosomal gel appears to be a potential platform for long-term topical antifungal therapy, offering improved drug retention, reduced dosing frequency, and increased patient compliance.</p>

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Preparation, Characterization and Evaluation of Griseofulvin-Loaded Transferosomal Gel for Sustained Drug Delivery

  • Mohammed Rahamathulla,
  • Suhas N S,
  • T Yunus Pasha,
  • Ali Alamri,
  • Yahya Alhamhoom,
  • Hanan Albataineh,
  • Sheetal Buddhadev,
  • Mohammed Muqtader Ahmed

摘要

Griseofulvin, a common antifungal, suffers from poor solubility and skin penetration, limiting its topical efficacy. The main purpose of the study is to develop and characterize a griseofulvin-loaded transfersomal gel to enhance topical delivery and sustain antifungal activity. The transfersomes were prepared by thin-film hydration with varying ratios of lecithin and Tween 80 and evaluated for vesicle size, morphology, and entrapment efficiency (EE). The optimized formulation (GRF7) had the highest EE (98.02 ± 0.55%) and the smallest nanosized spherical vesicles (167.32 ± 0.51 nm), as confirmed by scanning electron microscopy (SEM). The GRF7 transfersomes were combined with a Carbopol 934 gel basis and tested for pH, homogeneity, spreadability, drug content, viscosity, in vitro release, kinetic release, and stability. The gel’s physicochemical parameters were acceptable, with a pH of 6.78 ± 0.42, viscosity of 31,700 cps, and homogeneous drug content (97.98 ± 0.55%). In vitro diffusion experiments indicated sustained release (90.2% from the improved formulation, GRF-7) for 18 h. The release kinetics were consistent with the Korsmeyer-Peppas model (R²=0.996), suggesting a super case-II transport mechanism suitable for sustained-release topical systems. Over three months of short-term stability tests, there was no significant variation in pH, drug content, or release behavior. Overall, the griseofulvin-loaded transferosomal gel appears to be a potential platform for long-term topical antifungal therapy, offering improved drug retention, reduced dosing frequency, and increased patient compliance.