ArticleThe Journal of pharmacy and pharmacology2014
Monocarboxylate transporter mediated uptake of moxifloxacin on human retinal pigmented epithelium cells.
Article in The Journal of pharmacy and pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
1 citing paper in PubMed, 10 citations in OpenAlex.
- Roles of Drug Transporters in Blood-Retinal Barrier.Advances in experimental medicine and biology · 2019Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
objectivesThis work was aim to determine in vitro interaction of moxifloxacin with monocarboxylate transporter (MCT) using a human retinal pigment epithelium cells (ARPE-19).
methodsIn vitro moxifloxacin uptakes were performed at 37°C across ARPE-19 cells. Concentration-dependent uptake of moxifloxacin was performed to delineate moxifloxacin kinetics with MCT. Effects of MCT substrates, MCT inhibitors, pH and metabolic inhibitors on moxifloxacin uptake were conducted to delineate mechanism of moxifloxacin influx via MCT. KEY
findingsMoxifloxacin uptake was found to exhibit saturable kinetics (K(m) = 1.56 ± 0.32 μM and V(max) = 0.58 ± 0.16 μM/min/mg protein). Higher uptake of moxifloxacin was observed at acidic pH. MCT substrates such as salicylic acid, ofloxacin and L-lactic acid significantly inhibited the uptake of moxifloxacin. Furthermore, moxifloxacin uptake was significantly reduced in the presence of metabolic and MCT inhibitors. Overall, this study demonstrated an interaction of moxifloxacin with Na⁺ and H⁺-coupled transporter, most likely MCT1.
conclusionsApart from the lipophilicity, we anticipate that lowest vitreal half-life of intravitreal moxifloxacin compared with other fluoroquinolones may be due to its interaction with MCT. This information might be crucial in clinical settings and can be further explored to improve vitreous half-life and therapeutic efficacy of moxifloxacin.
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