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Antifungal activity and toxicity of an octyl gallate-loaded nanostructured lipid system on cells and nonmammalian animals

2022; Future Medicine; Volume: 17; Issue: 4 Linguagem: Inglês

10.2217/fmb-2021-0095

1746-0921

Júnya de Lacorte Singulani, Liliana Scorzoni, Patrícia Bento da Silva, Ana Carolina Nazaré, Carlos Roberto Polaquini, Franciele Garcia Baveloni, Marlus Chorilli, Luís Octávio Regasini, Ana Marisa Fusco‐Almeida, Maria José Soares Mendes‐Giannini,

Coconut Research and Applications

Aim: Octyl gallate (OG) loaded into a nanostructured lipid system (NLS) was tested for antifungal activity and in vitro and in vivo toxicity. Methods & Results: The features of NLS-OG were analyzed by dynamic light scattering and showed adequate size (132.1 nm) and homogeneity (polydispersity index = 0.200). OG was active against Paraccoccidioides spp., and NLS-OG did not affect antifungal activity. NLS-OG demonstrated reduced toxicity to lung cells and zebrafish embryos compared with OG, whereas NLS was toxic to hepatic cells. OG and NLS-OG did not show toxicity in a Galleria mellonella model at 20 mg/kg. All toxic concentrations were superior to MIC (antifungal activity). Conclusion: These results indicate good anti-Paracoccidioides activity and low toxicity of NLS-OG.Plain language summary Drugs for the treatment of fungal diseases are limited in number and present side effects, drug interactions, risks for pregnant women and fungal resistance. The authors produced a derivative compound from plants called octyl gallate (OG) and then incorporated it into a nanoparticle lipid system (NLS) for better distribution in biological fluids. NLS-OG was tested against a fungus called Paracoccidioides, which causes lung infections. The toxicity profile of NLS-OG was also evaluated in lung and hepatic cells as well as novel animal models. NLS-OG presented good antifungal activity and low toxicity in lung cells and embryos.