Voriconazole Loaded Spanlastics: Design, Formulation, Optimization, and Randomized Controlled Clinical Insights for...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Mycology

Background:

• Vulvovaginal candidiasis (VVC) is a common fungal infection.
• Voriconazole is a potent antifungal, but current delivery methods have limitations.
• There is a need for improved VVC treatment options with better safety and efficacy.

Purpose of the Study:

• To develop and characterize voriconazole-loaded spanlastics for VVC treatment.
• To evaluate the in vitro and ex vivo performance of the optimized formulation.
• To assess the clinical safety and efficacy of the voriconazole-loaded spanlastic gel compared to a market product.

Main Methods:

• A 3^2-factorial design was used to optimize voriconazole-loaded spanlastics.
• Characterization included entrapment efficiency, vesicle size, PDI, zeta potential, TEM, FTIR, and in vitro antifungal assays.
• Ex vivo permeation studies and a randomized controlled clinical trial were conducted.

Main Results:

• The optimized spanlastic system showed high entrapment efficiency (74.31%), optimal vesicle size (246.4 nm), and good stability.
• In vitro studies confirmed voriconazole's potent antifungal activity against Candida species.
• The spanlastic gel demonstrated a 1.3-fold enhancement in vaginal mucosa permeation and comparable clinical efficacy and safety to clotrimazole.

Conclusions:

• Optimized voriconazole-loaded spanlastic gel is a promising alternative for VVC treatment.
• The novel delivery system offers enhanced permeation and comparable clinical outcomes to existing therapies.
• This formulation presents a safe and effective option for managing vaginal candidiasis.