Abstract
Pipemidic acid (HPPA) is a quinolone antibacterial agent used mostly to treat gram-negative infections of the urinary tract, but its therapeutic use is limited because of its low solubility. Thus, to improve drug solubility, natural cyclodextrins (CDs) are used for their ability of including guest molecules within their cavities. The aim of this work was to evaluate the antibacterial activity and the preliminary anticancer activity of HPPA included into Heptakis (2,3,6-tri-O-methyl)-β-cyclodextrin (TRIMEB) as a possible approach for a new innovative formulation. The inclusion complex of HPPA with TRIMEB was prepared in solid state by the kneading method and confirmed by FT-IR and powered X-ray diffraction. The association in aqueous solutions of pipemidic acid with TRIMEB was investigated by UV-Vis spectroscopy. Job’s plots have been drawn by UV-visible spectroscopy to confirm the 1:1 stoichiometry of the host–guest assembly. The antibacterial activity of HPPA, TRIMEB and of their complex was tested on Escherichia coli, Pseudomonas aeruginosa, and Staphilococcus aureus. The complex was able to increase 47.36% of the median antibacterial activity of the free HPPA against E. coli (IC50 = 249 µM vs. 473 µM). Furthermore, these samples were tested on HepG-2 and MCF-7. After 72 h, the median tumoral cytotoxicity exerted by the complex was increased by 78.08% and 94.27% for HepG-2 and MCF-7 respectively, showing a stronger bioactivity of the complex than the single HAPPA.
Highlights
The discoveries about the quinolone class of antimicrobial agents evolved along the years
Similar to a previous study of Iacovino et al, 2013 [18] who evaluated the antibacterial activity and the tumoral cytotoxicity of the pipemidic acid (HPPA) complexed with the natural β-CD, we studied the antimicrobial and the antitumoral activities of HPPA complexed with TRIMEB
The initial assessment of the inclusion of HPPA into TRIMEB is based on the Fourier Transform Infrared (FT-IR) spectroscopy studies
Summary
The discoveries about the quinolone class of antimicrobial agents evolved along the years. Quinolones are molecules produced by synthesis showing, in their evolution, differences in activity because of various substituents added to the quinolone nucleus These antimicrobial agents have been classified from the first-generation to the fourth-generation quinolones going from molecules effective against aerobic gram-negative bacteria to molecules with an improved activity against gram-positive bacteria and anaerobes. Despite their unfavorable physico-chemical profiles, quinolones might have good opportunities to offer new compounds, especially selecting molecules with greater activity against infections difficult to treat and with lesser patient adverse reactions; at the moment, the main concern for the clinical use of quinolones is the bacterial resistance to these agents
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