CONICET | Buscador de Institutos y Recursos Humanos

Vaginal candidiasis is an opportunistic mucosal infection that affects women and is the second most common cause of vaginitis after bacterial vaginosis. Among different Candida species triggering this disease, C. albicans is the most predominant yeast causing vaginal candidiasis. It is commonly treated using azole antifungals, such as fluconazole, miconazole, itraconazole, clotrimazole, econazole, ketoconazole, or tioconazole. Tioconazole (TCZ), an imidazole antifungal agent, exhibits a broad spectrum of activity against a variety of microorganisms, and a higher activity against C. albicans than others azoles. Therefore, it is often used for the topical treatment of superficial mycoses and for the treatment of vaginal candidiasis.A critical challenge in pharmaceutical sciences is the design of drug delivery systems such as nanocapsules, which additionally are able to protect the drug from chemical or enzymatic degradation. The aim of the study was to produce a novel TCZ loaded chitosan nanocapsule delivery system and to characterize it for its suitability in vaginal application.The capsules were characterized for their size (146.8±0.8 nm) and zeta potential (+24.7±1.1 mV) using dynamic light scattering. The encapsulation efficiency (99.0%) was determined using HPLC. In-vitro release studies indicated 60% of relative release of the loaded drug within 24 h in simulated vaginal fluid. Long-term stability of the nanocapsules was confirmed by monitoring the size, polydispersity index, and zeta potential over a period of two months. Finally, in our study we successfully showed a higher fungicidal activity of TCZ loaded nanocapsules against C.albicans as compared to a suspension or solution of TCZ. Importantly, the minimum fungicidal concentration was found to be below the cytotoxic threshold of the drug-loaded capsules.The obtained results are essential for the development of a new pharmaceutical dosage form suitable for the treatment of vaginal candidiasis.