Novel Micelle Formulations to Increase Cutaneous Bioavailability of Azole Antifungals

The study aimed to enhance the delivery of azole antifungals to the skin by developing aqueous micelle solutions using novel block copolymers. Clotrimazole (CLZ), econazole nitrate (ECZ), and fluconazole (FLZ) were formulated into micelles, with ECZ showing the highest loading efficiency at 98.3%. The optimal ECZ-loaded micelle formulation (1.3 mg/mL; dn < 40 nm) significantly increased drug deposition in both porcine and human skin compared to a commercial cream, with over 13-fold and 7.5-fold improvements, respectively. Confocal microscopy suggested that the enhanced delivery was partly due to increased follicular penetration. The study concluded that MPEG-dihexPLA micelles substantially improve cutaneous bioavailability of ECZ, potentially leading to better clinical outcomes and the possibility of targeting hair follicles in future research.