Clotrimazole nanoparticle gel for mucosal administration

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Mycology

Background:

• Fungal infections of the oral and vaginal mucosa require effective topical treatments.
• Developing stable and bioavailable drug delivery systems is crucial for mucosal drug delivery.
• Clotrimazole (CLO) is a widely used antifungal agent, but its formulation impacts efficacy.

Purpose of the Study:

• To develop and compare clotrimazole (CLO)-loaded semisolid formulations based on monoolein aqueous dispersion (MAD) and nanostructured lipid carriers (NLC).
• To evaluate the physicochemical properties, drug release, and anticandidal activity of these novel formulations for mucosal application.

Main Methods:

• Characterization of MAD and NLC using cryogenic Transmission Electron Microscopy (cryo-TEM) and Photon Correlation Spectroscopy (PCS).
• Quantification of CLO entrapment efficiency and recovery using Sedimentation Field Flow Fractionation (SdFFF) coupled with HPLC.
• Rheological evaluation of viscosized formulations and in vitro drug diffusion studies using Franz cells.
• Anticandidal activity assessment against Candida albicans.

Main Results:

• High entrapment efficiency of CLO was achieved in both MAD and NLC.
• Viscosized MAD and NLC formulations exhibited suitable rheological properties for mucosal application.
• CLO diffusion rates from MAD and NLC were comparable to a commercial product (Canesten®).
• Both CLO-MAD and CLO-NLC demonstrated superior anticandidal activity against Candida albicans compared to free CLO.

Conclusions:

• Novel semisolid formulations of clotrimazole using MAD and NLC are suitable for oral and vaginal mucosal delivery.
• These formulations offer improved drug release and enhanced antifungal efficacy.
• MAD and NLC represent promising platforms for developing advanced topical antifungal treatments.