Antifungal activity of farnesol incorporated in liposomes and associated with fluconazole.

Autor: Bezerra CF; Department of Pharmaceutical Sciences, Federal University of Pernambuco- UFPE, Recife, PE, Brazil., de Alencar Júnior JG; Department of Pharmacy, Federal University of Ceará- UFC, Fortaleza, CE, Brazil., de Lima Honorato R; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil., Dos Santos ATL; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil., Pereira da Silva JC; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil., Gusmão da Silva T; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil., Leal ALAB; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil., Rocha JE; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil., de Freitas TS; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil., Tavares Vieira TA; Department of Pharmaceutical Sciences, Federal University of Pernambuco- UFPE, Recife, PE, Brazil; Department of Pharmacy, Federal University of Ceará- UFC, Fortaleza, CE, Brazil; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil; Faculty of Medicine of Juazeiro do Norte- Estácio FMJ, Juazeiro do Norte- CE, Brazil; Department of Pharmacy, Federal University of Paraíba- UFPB, João Pessoa, PB, Brazil; Gonçalo Moniz Institute, Oswaldo Cruz Foundation, Salvador, Bahia, Brazil; Department of Antibiotics, Federal University of Pernambuco- UFPE, Recife, PE, Brazil., Bezerra MCF; Faculty of Medicine of Juazeiro do Norte- Estácio FMJ, Juazeiro do Norte- CE, Brazil., Sales DL; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil., Kerntopf MR; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil., de Araujo Delmondes G; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil., Filho JMB; Department of Pharmacy, Federal University of Paraíba- UFPB, João Pessoa, PB, Brazil., Peixoto LR; Department of Pharmacy, Federal University of Paraíba- UFPB, João Pessoa, PB, Brazil., Pinheiro AP; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil., Ribeiro-Filho J; Gonçalo Moniz Institute, Oswaldo Cruz Foundation, Salvador, Bahia, Brazil., Coutinho HDM; Department of Biological Chemistry, Regional University of Cariri- URCA, Crato, CE, Brazil. Electronic address: hdmcoutinho@gmail.com., Morais-Braga MFB; Department of Biological Sciences, Regional University of Cariri- URCA, Crato, CE, Brazil., Gonçalves da Silva T; Department of Antibiotics, Federal University of Pernambuco- UFPE, Recife, PE, Brazil.
Jazyk: angličtina
Zdroj: Chemistry and physics of lipids [Chem Phys Lipids] 2020 Nov; Vol. 233, pp. 104987. Date of Electronic Publication: 2020 Oct 12.
DOI: 10.1016/j.chemphyslip.2020.104987
Abstrakt: Candida infections represent a threat to human health. Candida albicans is the main causative agent of invasive candidiasis, especially in immunosuppressed patients. The emergence of resistant strains has required the development of new therapeutic strategies. In this context, the use of liposomes as drug carrier systems is a promising alternative in drug development. Thus, considering the evidence demonstrating that sesquiterpene farnesol is a bioactive compound with antifungal properties, this study evaluated the activity farnesol-containing liposomes against different Candida strains. The IC 50 of farnesol and its liposomal formulation was assessed in vitro using cultures of Candida albicans, Candida tropicalis, and Candida krusei. The Minimum Fungicidal Concentration (MFC) was established by subculture in solid medium. The occurrence of fungal dimorphism was analyzed using optical microscopy. The effects on antifungal resistance to fluconazole were assessed by evaluating the impact of combined therapy on the growth of Candida strains. The characterization of liposomes was carried out considering their vesicular size, polydispersion index, and zeta medium potential, in addition to electron microscopy analysis. Farnesol exerted an antifungal activity that might be associated with the inhibition of fungal dimorphism, especially in Candida albicans. The incorporation of farnesol into liposomes significantly increased its antifungal activity against C. albicans, C. tropicalis, and C. krusei. In addition, liposomal farnesol potentiated the action of fluconazole against C. albicans and C. tropicalis. On the other hand, the association of unconjugated farnesol with fluconazole resulted in antagonistic effects. In conclusion, farnesol-containing liposomes have the potential to be used in antifungal drug development. However, further research is required to investigate how the antifungal properties of farnesol are affected by the interaction with liposomes, contributing to the modulation of antifungal resistance to conventional drugs.
(Copyright © 2020 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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