Synthesis, physicochemical characterization, toxicity and efficacy of a PEG conjugate and a hybrid PEG conjugate nanoparticle formulation of the antibiotic moxifloxacin

Tshweu, Lesego; Shemis, Mohamed; Abdelghany, Aya; Gouda, Abdullah E.; Pilcher, Lynne A.; Sibuyi, Nicole Remaliah Samantha; Meyer, Mervin; Balogun, Mohammed

doi:10.1039/c9ra10872f

Cited by 18 publications

(15 citation statements)

References 27 publications

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“…Bacterial growth was further evaluated by Alamar Blue colorimetric assay (Invitrogen, Eugene, Oregon, USA), where 10 µL of the dye was added to each well and incubated for 3 hr. The blue color was converted to a pink-purplish color by live bacteria that was quantifiable by measuring absorbance at 570 nm and a reference wavelength at 700 nm [83].…”

Section: Minimum Inhibitory Concentration (Mic)mentioning

confidence: 99%

Broad Spectrum Anti-Bacterial Activity and Non-Selective Toxicity of Gum Arabic Silver Nanoparticles

Fadaka

Meyer

Ahmed

et al. 2022

IJMS

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Silver nanoparticles (AgNPs) are the most commercialized nanomaterials and presumed to be biocompatible based on the biological effects of the bulk material. However, their physico-chemical properties differ significantly to the bulk materials and are associated with unique biological properties. The study investigated the antimicrobial and cytotoxicity effects of AgNPs synthesized using gum arabic (GA), sodium borohydride (NaBH4), and their combination as reducing agents. The AgNPs were characterized using ultraviolet-visible spectrophotometry (UV-Vis), dynamic light scattering (DLS), transmission electron microscopy (TEM), and Fourier-transform infrared spectroscopy (FT-IR). The anti-bacterial activity was assessed using agar well diffusion and microdilution assays, and the cytotoxicity effects on Caco-2, HT-29 and KMST-6 cells using MTT assay. The GA-synthesized AgNPs (GA-AgNPs) demonstrated higher bactericidal activity against all bacteria, and non-selective cytotoxicity towards normal and cancer cells. AgNPs reduced by NaBH4 (C-AgNPs) and the combination of GA and NaBH4 (GAC-AgNPs) had insignificant anti-bacterial activity and cytotoxicity at ≥50 µg/mL. The study showed that despite the notion that AgNPs are safe and biocompatible, their toxicity cannot be overruled and that their toxicity can be channeled by using biocompatible polymers, thereby providing a therapeutic window at concentrations that are least harmful to mammalian cells but toxic to bacteria.

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Section: Minimum Inhibitory Concentration (Mic)mentioning

confidence: 99%

Broad Spectrum Anti-Bacterial Activity and Non-Selective Toxicity of Gum Arabic Silver Nanoparticles

Fadaka

Meyer

Ahmed

et al. 2022

IJMS

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“…Various delivery system architectures and formulations, including polymeric nanoparticles, magnetic nanoparticles, liposomes, emulsions, cyclodextrin complexes, and polymer–drug conjugates have been reported [ 30 ]. In particular, polymer–drug conjugates are of interest because a hydrophilic polymer such as polyethylene glycol (PEG) creates a new water-soluble chemical entity [ 31 ]. In contrast, liposomes and nanoemulsions are thermodynamically stable biphasic aqueous solutions of drug-containing solids.…”

Section: Introductionmentioning

confidence: 99%

Anti-Cancer and Immunomodulatory Activity of a Polyethylene Glycol-Betulinic Acid Conjugate on Pancreatic Cancer Cells

Fru

Nweke

Mthimkhulu

et al. 2021

Life

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Drug delivery systems involving polymer therapeutics enhance drug potency by improved solubility and specificity and may assist in circumventing chemoresistance in pancreatic cancer (PC). We compared the effectiveness of the naturally occurring drug, betulinic acid (BA), alone and in a polymer conjugate construct of polyethylene glycol (PEG), (PEG–BA), on PC cells (MIA PaCa-2), a normal cell line (Vero) and on peripheral blood mononuclear cells (PBMCs). PEG–BA, was tested for its effect on cell death, immunomodulation and chemoresistance-linked signalling pathways. The conjugate was significantly more toxic to PC cells (p < 0.001, IC50 of 1.35 ± 0.11 µM) compared to BA (IC50 of 12.70 ± 0.34 µM), with a selectivity index (SI) of 7.28 compared to 1.4 in Vero cells. Cytotoxicity was confirmed by increased apoptotic cell death. PEG–BA inhibited the production of IL-6 by 4–5.5 fold compared to BA-treated cells. Furthermore, PEG–BA treatment of MIA PaCa-2 cells resulted in the dysregulation of crucial chemoresistance genes such as WNT3A, TXNRD1, SLC2A1 and GATA3. The dysregulation of chemoresistance-associated genes and the inhibition of cytokines such as IL-6 by the model polymer construct, PEG–BA, holds promise for further exploration in PC treatment.

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“…Eventually, hemolysis (%) was determined by the following equation; 27 The antimicrobial activity of synthesized NPs was performed using ager well diffusion method with some modications. [28][29][30][31] For this assay, inoculums of selected strain were used with optical density (OD) between 0.1-0.5 at 600 nm. The inoculum was spread evenly on nutrient agar plates, wells of 70 mm 2 diameter were bored and selected concentrations of NPs solution was added into the well.…”

Section: Biocompatibilitymentioning

confidence: 99%

Development of bactericidal spinel ferrite nanoparticles with effective biocompatibility for potential wound healing applications

et al. 2021

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Synthesis, physicochemical characterization, toxicity and efficacy of a PEG conjugate and a hybrid PEG conjugate nanoparticle formulation of the antibiotic moxifloxacin

Abstract: Moxifloxacin was conjugated to polyethylene glycol to segregate host cell toxicity from antimicrobial activity. The conjugate was then encapsulated into a polycaprolactone nanoparticle to assist the simultaneous delivery of multiple drugs to the site of microbial infection.

Cited by 18 publications

References 27 publications

Broad Spectrum Anti-Bacterial Activity and Non-Selective Toxicity of Gum Arabic Silver Nanoparticles

Broad Spectrum Anti-Bacterial Activity and Non-Selective Toxicity of Gum Arabic Silver Nanoparticles

Anti-Cancer and Immunomodulatory Activity of a Polyethylene Glycol-Betulinic Acid Conjugate on Pancreatic Cancer Cells

Development of bactericidal spinel ferrite nanoparticles with effective biocompatibility for potential wound healing applications

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