Interaction between different pharmaceutical excipients in liquid dosage forms—assessment of cytotoxicity and antimicrobial activity

Dániel Nemes, Renátó Kovács, Fruzsina Nagy, Mirtill Mez o, Nikolett Poczok, Zoltán Ujhelyi, Agota Pet o, Pálma Fehér, Ferenc Fenyvesi, J. Váradi, M. Vecsernyés, I. Bácskay

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Nowadays, the safety of parabens as pharmaceutical preservatives is debated. Recent studies investigated their interference with the oestrogen receptors, nevertheless their carcinogenic activity was also proved. That was the reason why the re-evaluation of the biocompatibility and antimicrobial activity of parabens is required using modern investigation methods. We aimed to test the cytotoxic, antifungal and antibacterial effect of parabens on Caco-2 cells, C. albicans, C. parapsilosis, C. glabrata, E. coli, P. aeruginosa and S. aureus. Two complex systems (glycerol—Polysorbate 20; ethanol—Capryol PGMC™) were formulated to study—with the MTT-assay and microdilution method, respectively—how other excipients may modify the biocompatibility and antimicrobial effect of parabens. In the case of cytotoxicity, the toxicity of these two systems was highly influenced by co-solvents and surfactants. The fungi and bacteria had significantly different resistance in the formulations and in some cases the excipients could highly modify the effectiveness of parabens both in an agonistic and in a counteractive way. These results indicate that with appropriate selection, non-preservative excipients can contribute to the antimicrobial safety of the products, thus they may decrease the required preservative concentration.

Original languageEnglish
Article number1827;
JournalMolecules
Volume23
Issue number7
DOIs
Publication statusPublished - Jan 1 2018

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Keywords

  • Caco-2 cells
  • Cytotoxicity
  • Excipient interaction
  • Liquid dosage forms
  • Preservative
  • Surfactant

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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