Human THP-1 monocyte uptake and cellular disposition of 14C-grepafloxacin

Hall, Iris H.; Schwab, Ute; Ward, E. Stacy; Rublein, John; Butts, John D.; Ives, Timothy J.

doi:10.1007/s10156-003-0289-8

Cited by 2 publications

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“…Confocal laser scanning microscopy was performed in order to assess the intracellular localization of the cargo carried by P14 unimolecular micelles. Differentiated THP-1 macrophages were incubated for 1 h with P14 unimolecular micelles, loaded with Oregon-green (100 μg/mL) (Figure ). A Z -stack acquisition performed with Carl Zeiss LSM 700 BW microscope allowed acquiring zoom and X / Y axes sections of the immobilized differentiated THP-1 macrophages.…”

Section: Resultsmentioning

confidence: 99%

“…For cellular uptake studies, THP-1 cells (3 × 10 5 cells per well) were differentiated in an 8-well glass bottom μ-slide (ibidi, Germany) for 24 h at 37°C, 5% CO 2 . Cell medium was removed and cells were then treated with fresh medium containing Oregon-green (100 μg/mL) loaded P14 unimolecular micelles and incubated for 1 h. 26 Cells nuclei were stained with Hoechst 33342 dye (1 μg/mL, ThermoFisher). F-actin was stained with Alexa Fluor 647 Phalloidin (1 μg/mL, ThermoFisher) or alternatively the cells membrane was stained with deep red CellMask (1 μg/mL, Life Technologies).…”

Section: ■ Experimental Sectionmentioning

confidence: 99%

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Biocompatible Unimolecular Micelles Obtained via the Passerini Reaction as Versatile Nanocarriers for Potential Medical Applications

et al. 2018

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A Passerini three-component polymerization was performed for the synthesis of amphiphilic star-shaped block copolymers with hydrophobic cores and hydrophilic coronae. The degree of polymerization of the hydrophobic core was varied from 5 to 10 repeating units, and the side chain ends were conjugated by performing a Passerini-3CR with PEG-isocyanide and PEG-aldehyde (950 g/mol). The resulting amphiphilic star-shaped block copolymers contained thioether groups, which could be oxidized to sulfones in order to further tune the polarity of the polymer chains. The ability of the amphiphilic copolymers to act as unimolecular micellar encapsulants was tested with the water-insoluble dye Orange II, the water-soluble dye Para Red and the macrolide antibiotic azithromycin. The results showed that the new copolymers were able to retain drug cargo at pH levels corresponding to circulating blood and selectively release therapeutically effective doses of antibiotic as measured by bacterial cell kill. The polymers were also well-tolerated by differentiated THP-1 macrophages in the absence of encapsulated drugs.

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Section: Resultsmentioning

confidence: 99%

Section: ■ Experimental Sectionmentioning

confidence: 99%

Biocompatible Unimolecular Micelles Obtained via the Passerini Reaction as Versatile Nanocarriers for Potential Medical Applications

et al. 2018

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Fluoroquinolones and tendon disorders

Melhus¹

2005

Expert Opinion on Drug Safety

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Fluoroquinolones are the most potent oral antibiotics in clinical use today. Increasingly, these drugs are being prescribed for relatively benign infections and for new categories of patients, including paediatric patients. As their use becomes more frequent, so will the adverse events. This review focuses on a rare but debilitating adverse reaction, the fluoroquinolone-associated tendinopathy. Despite many published case reports and approximately 3500 cases reported to the World Health Organization Collaborating Centre for Drug Monitoring, little is known about the mechanisms behind this fluoroquinolone-specific toxicity. Data on chemical properties, mode of action, pharmacokinetic features, clinical presentation and risk factors in relation to tendon toxicity are discussed and the literature reviewed. As long as the musculoskeletal toxicity cannot be predicted by in vitro or in vivo models and this class of antibiotics is one of the most commonly linked to selection of resistant bacteria, a more prudent use of fluoroquinolones is warranted.

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Human THP-1 monocyte uptake and cellular disposition of 14C-grepafloxacin

Cited by 2 publications

References 27 publications

Biocompatible Unimolecular Micelles Obtained via the Passerini Reaction as Versatile Nanocarriers for Potential Medical Applications

Biocompatible Unimolecular Micelles Obtained via the Passerini Reaction as Versatile Nanocarriers for Potential Medical Applications

Fluoroquinolones and tendon disorders

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