Ketoconazole/calix[n]arenes-based compounds improve the antifungal activity against azole-resistant Candida isolates - 18/05/22
Abstract |
Ketoconazole (KTZ) is an antifungal agent; however, its bioavailability and therapeutic efficacy are reduced by the low aqueous solubility of the drug. Aiming at providing to improve the biopharmaceutical properties of KTZ, we studied the water-soluble different calix[n]arenes as carrier systems for KTZ. All calix[n]arene-KTZ tested showed in vitro antifungal activity superior or similar to free KTZ against Candida spp. The CX6Na/KTZ obtained by physical mixture and freeze-drying methods were the most active, decreasing KTZ concentrations required for growth inhibition against azole-resistant isolates (e.g., C. auris). Moreover, CX6Na/KTZ showed no toxic effect on Galleria mellonella larvae and the treatment of infected larvae with C. albicans and C. auris was effective at a lower dose compared with free KTZ. Thus, CX6Na/KTZ may have a potential approach to treat mycosis, especially by improvement of KTZ inhibitory activity against azole-resistant Candida.
El texto completo de este artículo está disponible en PDF.Keywords : Drug carrier, Imidazole, Candida auris, in vivo studies, Galleria mellonella
Esquema
Vol 32 - N° 2
Artículo 101254- mai 2022 Regresar al númeroBienvenido a EM-consulte, la referencia de los profesionales de la salud.
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