Abstract

In the era of antimicrobial resistance, the identification of new antimicrobials is a research priority at the global level. In this regard, the attention towards functional antimicrobial polymers, with biomedical/pharmaceutical grade, and exerting anti-infective properties has recently grown. The aim of this study was to evaluate the antibacterial, antibiofilm, and antiadhesive properties of a number of quaternized chitosan derivatives that have displayed significant muco-adhesive properties and wound healing promotion features in previous studies. Low (QAL) and high (QAH) molecular weight quaternized chitosan derivatives were synthetized and further modified with thiol moieties or pendant cyclodextrin, and their antibacterial activity evaluated as minimal inhibitory concentrations (MIC) and minimal bactericidal concentrations (MBC). The ability of the derivatives to prevent biofilm formation was assessed by crystal violet staining. Both QAL and QAH derivatives exerted a bactericidal and/or inhibitory activity on the growth of P. aeruginosa and S. epidermidis. The same compounds also showed marked dose-dependent anti-biofilm activity. Furthermore, the high molecular weight derivative (QAH) was used to functionalize titanium plates. The successful functionalization, demonstrated by electron microscopy, was able to partially inhibit the adhesion of S. epidermidis at 6 h of incubation. The shown ability of the chitosan derivatives tested to both inhibit bacterial growth and/or biofilm formation of clinically relevant bacterial species reveals their potential as multifunctional molecules against bacterial infections.

Highlights

  • Nowadays, the rapid and worldwide spread of antimicrobial resistance represents one of the major threats to public health

  • The antibacterial activity of different Ch-derivatives was tested against exponentially growing P. aeruginosa and S. epidermidis in terms of minimal inhibitory concentration (MIC) values and by measuring the optical density of bacterial suspensions exposed to different concentrations of the compounds for 24 h

  • QAH and QAH-Pro caused a dose-dependent reduction of the OD590 of P. aeruginosa with a complete inhibition of visible bacterial growth (MIC value) at the concentration of 0.31 and 0.15 mg/mL, respectively (Table 2, Figure 1A)

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Summary

Introduction

The rapid and worldwide spread of antimicrobial resistance represents one of the major threats to public health. Worldwide increase in life expectancy and the advances in medical technology have led to a greater demand for medical implants and a rising number of implant-associated infections that account for over half of all health-care associated infections. The list of bacterial species causing device-associated infection is quite heterogeneous, but most frequently it includes the Gram-positive staphlylococci (both S. aureus and S. epidermidis), and the Gram-negative Pseudomonas aeruginosa. This latter is an environmental opportunistic bacterium recently classified as a priority pathogen for the research and development of novel antimicrobials due to its increasing antibiotic resistance and its relevance in health care-associated infections [8]

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