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Carbohydr Polym. 2016 Nov 5;152:672-678. doi: 10.1016/j.carbpol.2016.07.013. Epub 2016 Jul 16.

Enhanced inhibition of bacterial biofilm formation and reduced leukocyte toxicity by chloramphenicol:β-cyclodextrin:N-acetylcysteine complex.

Author information

1
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina; Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET, Universidad Nacional de Córdoba, Córdoba, Argentina. Electronic address: aiassa@fcq.unc.edu.ar.
2
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina; Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET, Universidad Nacional de Córdoba, Córdoba, Argentina. Electronic address: ariana@fcq.unc.edu.ar.
3
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina; Instituto Multidisciplinario de Biología Vegetal (IMBIV), CONICET, Universidad Nacional de Córdoba, Córdoba, Argentina. Electronic address: becerra@fcq.unc.edu.ar.
4
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina; Instituto Multidisciplinario de Biología Vegetal (IMBIV), CONICET, Universidad Nacional de Córdoba, Córdoba, Argentina. Electronic address: inesalbesa@fcq.unc.edu.ar.
5
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina; Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET, Universidad Nacional de Córdoba, Córdoba, Argentina. Electronic address: mrlcor@fcq.unc.edu.ar.

Abstract

The purpose of this study was to improve the physicochemical and biological properties of chloramphenicol (CP) by multicomponent complexation with β-cyclodextrin (β-CD) and N-acetylcysteine (NAC). The present work describes the ability of solid multicomponent complex (MC) to decrease biomass and cellular activity of Staphylococcus by crystal violet and XTT assay, and leukocyte toxicity, measuring the increase of reactive oxygen species by chemiluminescence, and using 123-dihydrorhodamine. In addition, MC was prepared by the freeze-drying or physical mixture methods, and then characterized by scanning electron microscopy and powder X-ray diffraction. Nuclear magnetic resonance and phase solubility studies provided information at the molecular level on the structure of the MC and its association binding constants, respectively. The results obtained allowed us to conclude that MC formation is an effective pharmaceutical strategy that can reduce CP toxicity against leukocytes, while enhancing its solubility and antibiofilm activity.

KEYWORDS:

Chloramphenicol; Microbiological activity; N-Acetylcysteine; Solubility; Toxicity; β-Cyclodextrin

PMID:
27516318
DOI:
10.1016/j.carbpol.2016.07.013
[Indexed for MEDLINE]

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