Membranes (Aug 2020)

Antifungal Properties of Nerolidol-Containing Liposomes in Association with Fluconazole

  • Camila Fonseca Bezerra,
  • José Geraldo de Alencar Júnior,
  • Rosilaine de Lima Honorato,
  • Antonia Thassya Lucas dos Santos,
  • Josefa Carolaine Pereira da Silva,
  • Taís Gusmão da Silva,
  • Antonio Linkoln Alves Borges Leal,
  • Thiago Sampaio de Freitas,
  • Thiago Adler Tavares Vieira,
  • Janaína Esmeraldo Rocha,
  • Débora Lima Sales,
  • José Maria Barbosa Filho,
  • Gabriela Ribeiro de Sousa,
  • Allyson Pontes Pinheiro,
  • Jaime Ribeiro-Filho,
  • Henrique Douglas Melo Coutinho,
  • Maria Flaviana Bezerra Morais-Braga,
  • Teresinha Gonçalves da Silva

DOI
https://doi.org/10.3390/membranes10090194
Journal volume & issue
Vol. 10, no. 9
p. 194

Abstract

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(1) Background: Infections by Candida species represent a serious threat to the health of immunocompromised individuals. Evidence has indicated that nerolidol has significant antifungal properties. Nonetheless, its use is restricted due to a low water solubility and high photosensitivity. The incorporation into liposomes may represent an efficient alternative to improve the physicochemical and biopharmaceutical properties of this compound. The present study aimed to characterize the antifungal properties of liposomal nerolidol, alone or in combination with fluconazole. Of note, this is the first study reporting the antifungal activity of liposomal nerolidol and its potentiating effect in association with fluconazole. (2) Methods: The Inhibitory Concentration 50%-IC50 and minimum fungicide concentrations (MFC) of the substances against Candida albicans (CA), Candida tropicalis (CT), and Candida krusei (CK) were established by subculture in a solid medium. To evaluate the antifungal-enhancing effect, the MFC of fluconazole was determined in the presence or absence of subinhibitory concentrations of nerolidol (free or liposomal). The analysis of fungal dimorphism was performed through optical microscopy and the characterization of liposomes was carried out considering the vesicular size, polydispersion index, and zeta medium potential, in addition to a scanning electron microscopy analysis. (3) Results: The physicochemical characterization revealed that liposomes were obtained as homogenous populations of spherical vesicles. The data obtained in the present study indicate that nerolidol acts as an antifungal agent against Candida albicans and Candida tropicalis, in addition to potentiating (only in the liposomal form) the effect of fluconazole. However, the compound had little inhibitory effect on fungal dimorphism. (4) Conclusions: The incorporation of nerolidol into liposomes improved its antifungal-modulating properties.

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