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Poloxamer-enhanced solubility of griseofulvin and its related antifungal activity against Trichophyton spp
Pittol, Vanessa; Veras, Kleyton Santos; Kaiser, Samuel; Danielli, Letícia Jacobi; Fuentefria, Alexandre Meneghello; Ortega, George González.
  • Pittol, Vanessa; Federal University of Rio Grande do Sul. Pharmacy Faculty. Laboratory of Galenic Development. Porto Alegre. BR
  • Veras, Kleyton Santos; Federal University of Rio Grande do Sul. Pharmacy Faculty. Laboratory of Galenic Development. Porto Alegre. BR
  • Kaiser, Samuel; Federal University of Rio Grande do Sul. Pharmacy Faculty. Laboratory of Galenic Development. Porto Alegre. BR
  • Danielli, Letícia Jacobi; Federal University of Rio Grande do Sul. Pharmacy Faculty. Laboratory of Pharmacognosy. Porto Alegre. BR
  • Fuentefria, Alexandre Meneghello; Federal University of Rio Grande do Sul. Pharmacy Faculty. Laboratory of Applied Mycology. Porto Alegre. BR
  • Ortega, George González; Federal University of Rio Grande do Sul. Pharmacy Faculty. Laboratory of Galenic Development. Porto Alegre. BR
Braz. J. Pharm. Sci. (Online) ; 58: e19731, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394038
ABSTRACT
Abstract Poorly water-soluble drugs, such as the antifungal drug griseofulvin (GF), exhibit limited bioavailability, despite their high membrane permeability. Several technological approaches have been proposed to enhance the water solubility and bioavailability of GF, including micellar solubilization. Poloxamers are amphiphilic block copolymers that increase drug solubility by forming micelles and supra-micellar structures via molecular self-association. In this regard, the aim of this study was to evaluate the water solubility increment of GF by poloxamer 407 (P407) and its effect on the antifungal activity against three Trichophyton mentagrophytes and two T. rubrum isolates. The GF water solubility profile with P407 revealed a non-linear behavior, well-fitted by the sigmoid model of Morgan-Mercer-Flodin. The polymer promoted an 8-fold increase in GF water solubility. Fourier-transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), and 2D nuclear magnetic resonance (NMR Roesy) spectroscopy suggested a GF-P407 interaction, which occurs in the GF cyclohexene ring. These results were supported by an increase in the water solubility of the GF impurities with the same molecular structure. The MIC values recorded for GF ranged from 0.0028 to 0.0172 mM, except for T. Mentagrophytes TME34. Notably, the micellar solubilization of GF did not increase its antifungal activity, which could be related to the high binding constant between GF and P407.
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Full text: Available Index: LILACS (Americas) Main subject: Solubility / Spectrum Analysis / Trichophyton / Poloxamer / Griseofulvin Language: English Journal: Braz. J. Pharm. Sci. (Online) Journal subject: Farmacologia / Terapˆutica / Toxicologia Year: 2022 Type: Article Affiliation country: Brazil Institution/Affiliation country: Federal University of Rio Grande do Sul/BR

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Full text: Available Index: LILACS (Americas) Main subject: Solubility / Spectrum Analysis / Trichophyton / Poloxamer / Griseofulvin Language: English Journal: Braz. J. Pharm. Sci. (Online) Journal subject: Farmacologia / Terapˆutica / Toxicologia Year: 2022 Type: Article Affiliation country: Brazil Institution/Affiliation country: Federal University of Rio Grande do Sul/BR