skip to main content
Idioma:

Development of inclusion complex based on cyclodextrin and oxazolidine derivative

Silva, Rafael Ramos ; Amorim, Cézar Augusto da Cruz ; Lima, Maria do Carmo Alves ; Rabello, Marcelo Montenegro ; Hernandes, Marcelo Zaldini ; Rêgo, Moacyr Jesus Barreto de Melo ; Pitta, Maira Galdino da Rocha ; Oliveira, Maria Danielly Lima de ; Andrade, César Augusto Souza de

Brazilian Journal of Pharmaceutical Sciences, 2023-01, Vol.59 [Periódico revisado por pares]

Universidade de São Paulo, Faculdade de Ciências Farmacêuticas

Texto completo disponível

Citações Citado por
  • Título:
    Development of inclusion complex based on cyclodextrin and oxazolidine derivative
  • Autor: Silva, Rafael Ramos ; Amorim, Cézar Augusto da Cruz ; Lima, Maria do Carmo Alves ; Rabello, Marcelo Montenegro ; Hernandes, Marcelo Zaldini ; Rêgo, Moacyr Jesus Barreto de Melo ; Pitta, Maira Galdino da Rocha ; Oliveira, Maria Danielly Lima de ; Andrade, César Augusto Souza de
  • Assuntos: Characterization ; Cyclodextrin ; Modeling ; Oxazolidine ; PHARMACOLOGY & PHARMACY ; Solubility
  • É parte de: Brazilian Journal of Pharmaceutical Sciences, 2023-01, Vol.59
  • Descrição: Abstract Oxazolidine derivatives (OxD) have been described as third-line antibiotics and antitumoral agents. The inclusion complexes based on cyclodextrin could improve the solubility and bioavailability of these compounds. A novel synthetic OxD was used, and its inclusion complexes were based on 2-hydroxy-beta-cyclodextrin (2-HPβCD). We conducted an in silico study to evaluate the interaction capacity between OxD and 2-HPβCD. Characterization studies were performed through scanning electron microscopy (SEM), Fourier-transformed infrared (FTIR), nuclear magnetic resonance spectroscopy (1H-NMR), X-ray diffraction (XRD), and thermal analyses. A kinetic study of the OxD was performed, including a cytotoxicity assay using peripheral blood mononuclear cells (PBMCs). The maximum increment of solubility was obtained at 70 mM OxD using 400 mM 2-HPβCD. SEM analyses and FTIR spectra indicated the formation of inclusion complexes. 1H-NMR presented chemical shifts that indicated 1:1 stoichiometry. Different thermal behaviors were obtained. The pharmacokinetic profile showed a short release time. Pure OxD and its inclusion complex did not exhibit cytotoxicity in PBMCs. In silico studies provided a foremost insight into the interactions between OxD and 2-HPβCD, including a higher solubility in water and an average releasing profile without toxicity in normal cells.
  • Editor: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
  • Idioma: Inglês;Português
Voltar para lista de resultados

  • Realização: ABCD-USP USP   Logos de Redes Sociais: Freepik

Buscando em bases de dados remotas. Favor aguardar.