Journal
JOURNAL DE MYCOLOGIE MEDICALE
Volume 32, Issue 2, Pages -Publisher
MASSON EDITEUR
DOI: 10.1016/j.mycmed.2022.101254
Keywords
Drug carrier; Imidazole; Candida auris; in vivo studies; Galleria mellonella
Categories
Funding
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2017/19,374-9]
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq) [405,556/2018-7]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]
- CNPq
- FAPESP [2018/12,149-2, 2018/03,708-8]
Ask authors/readers for more resources
Water-soluble calix[n]arenes can be used as carrier systems for KTZ to improve its biopharmaceutical properties. CX6Na/KTZ showed superior inhibitory activity against azole-resistant Candida compared to free KTZ, and had no toxic effects on Galleria mellonella larvae.
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]areneKTZ 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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available