Bacitracin-Conjugated Superparamagnetic Iron Oxide Nanoparticles: Synthesis, Characterization and Antibacterial Activity

Chemistry, East China Normal University, 3663 Zhongshan Road (N), Shanghai 200062 (P. R. China).
ChemPhysChem (Impact Factor: 3.42). 10/2012; 13(14):3388-96. DOI: 10.1002/cphc.201200161
Source: PubMed


Bacitracin-conjugated superparamagnetic iron oxide (Fe(3) O(4) ) nanoparticles were prepared by click chemistry and their antibacterial activity was investigated. After functionalization with hydrophilic and biocompatible poly(acrylic acid), water-soluble Fe(3) O(4) nanoparticles were obtained. Propargylated Fe(3) O(4) nanoparticles were then synthesized by carbodiimide reaction of propargylamine with the carboxyl groups on the surface of the iron oxide nanoparticles. By further reaction with N(3) -bacitracin in a Cu(I) -catalyzed azide-alkyne cycloaddition, the magnetic Fe(3) O(4) nanoparticles were modified with the peptide bacitracin. The functionalized magnetic nanoparticles were characterized by powder X-ray diffraction, X-ray photoelectron spectroscopy, TEM, zeta-potential analysis, FTIR spectroscopy and vibrating-sample magnetometry. Cell cytotoxicity tests indicate that bacitracin-conjugated Fe(3) O(4) nanoparticles show very low cytotoxicity to human fibroblast cells, even at relatively high concentrations. In view of the antibacterial activity of bacitracin, the biofunctionalized Fe(3) O(4) nanoparticles exhibit an antibacterial effect against both Gram-positive and Gram-negative organisms, which is even higher than that of bacitracin itself. The enhanced antibacterial activity of the magnetic nanocomposites allows the dosage and the side effects of the antibiotic to be reduced. Due to the antibacterial effect and magnetism, the bacitracin-functionalized magnetic nanoparticles have potential application in magnetic-targeting biomedical applications.

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    • "Therapeutic peptides used in such cases are of limited number i.e. daptomycin, vancomycin, polymixin, bacitracin, cyclosporin etc. Liposomal delivery systems for daptomycin and polymixin and some other model proteins/peptides have been developed showing their therapeutic potential in infectious diseases. Metal nanoparticles of Fe 2 O 3 and silver have also been prepared coated with bacitracin and/or polymixin E which have shown enhanced uptake of particles in bacterial cells and have demonstrated multiple mechanisms of antimicrobial activity which can be helpful in resistance [226] [227]. PLA/PLGA based nanoparticulate and micelle systems and cationic emulsion system have also been reported for cyclosporine A for providing long-lasting activity in ocular infection [228] [229] [230]. "
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    ABSTRACT: The advent of recombinant DNA technology and computational designing has fueled the emergence of proteins and peptides as a new class of modern therapeutics such as vaccines, antigens, antibodies and hormones. Demand for such therapeutics has increased recently due to their distinct pharmacodynamic characteristics of specificity of action and high potency. However, their potential clinical applications are often hindered by involvement of factors which impact their therapeutic potential negatively. Large size, low permeability, conformational fragility, immunogenicity, metabolic degradation and short half-life results in poor bioavailability and inferior efficacy. These challenges have encouraged researchers to devise strategies for effective delivery of proteins and peptides. Recent advances made in nanotechnology are being sought to overcome aforesaid problems and to offer advantages such as higher drug loading, improved stability, sustained release, amenability for non-parenteral administration and targeting through surface modifications. This review focuses on elaborating the role of nanotechnology based formulations and associated challenges in protein and peptide delivery, their clinical outlook and future perspective.
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    • ",WaterResearch(2014), antimicrobialactivity,thisworkhasrevealedtheopposite (OnaiziandLeong,2011).Inotherwords,theresultsobtained fortheMNP-PEG-immobilized(RW)3at500mM(Fig.5)revealed adecreaseofthemicrobialpopulationonbothstrains,indicatingabactericidaleffect ,while500mMoffreepeptideonly causedbacteriostaticeffectonEscherichiacoliK-12DSM498 (Fig.2).SimilarresultshavebeenreportedbyZhangandco- workers,whereironoxideMNPswerefunctionalizedwith bacitracin,displayingahigherantimicrobialactivitythan bacitracinalone(Zhangetal.,2012). "
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    • "Moreover, nanoparticles with smaller particle sizes have been shown to possess antimicrobial properties [4]. The antimicrobial activity of iron oxide nanoparticles has largely been studied against different organisms [1, 5–7] and has been shown to depend on three factors: size, stability, and concentration in the growth medium. The size of microbial cells is in the micrometer range while outer cellular membranes have pores in the nanometer range. "
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