ntifungal activity and toxicity of an octyl gallate-loaded nanostructured lipid system on cells and nonmammalian animal

Author(s)

Singulani, Junya L. ^{[1, 2]} ; Scorzoni, Liliana ^{[1, 3]} ; da Silva, Patricia B. ^[1] ; Nazare, Ana C. ^[4] ; Polaquini, Carlos R. ^[4] ; Baveloni, Franciele G. ^[1] ; Chorilli, Marlus ^[1] ; Regasini, Luis O. ^[4] ; Fusco-Almeida, Ana M. ^[1] ; Mendes-Giannini, Maria J. S. ^[1]

Affiliation

^[1] Sao Paulo State Univ, Sch Pharmaceut Sci, BR-14800903 Araraquara, SP - Brazil

^[2] Univ Fed Minas Gerais, Inst Biol Sci, BR-31270901 Belo Horizonte, MG - Brazil

^[3] Univ Guarulhos, Programa Posgrad Enfermagem, BR-07023070 Guarulhos, SP - Brazil

^[4] Sao Paulo State Univ, Inst Biosci, Humanities & Exact Sci, BR-15054000 Sao Jose Do Rio Preto, SP - Brazil

• Document type: Journal article
• Source: FUTURE MICROBIOLOGY; v. 17, n. 4, p. 281-291, MAR 2022.
• Web of Science Citations: 0

Abstract

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. 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. (AU)

• FAPESP's process: 14/10446-9 - Evaluation of new therapies and biomarkers in paracoccidioidomycosis: antifungal activity of alkyl gallates in alternative models and mice and identification of circulating microRNAs
• Grantee: Junya de Lacorte Singulani
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 17/06658-9 - Platform for antifungal development in a nanostructured lipid system aiming at efficacy and safety in alternative animal models
• Grantee: Junya de Lacorte Singulani
• Support Opportunities: Scholarships in Brazil - Post-Doctoral