Please use this identifier to cite or link to this item: http://repository.unizik.edu.ng/handle/123456789/473
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dc.contributor.authorMacDonald, Chris-
dc.contributor.authorShao, Di-
dc.contributor.authorOli, Angus-
dc.contributor.authorAgu, Remigius U.-
dc.date.accessioned2023-02-15T11:43:52Z-
dc.date.available2023-02-15T11:43:52Z-
dc.date.issued2013-
dc.identifier.citationJournal of Drug Targeting, 21(1): 97–106en_US
dc.identifier.issn1029-2330 online-
dc.identifier.issnISSN 1061-186X print-
dc.identifier.uriDOI: 10.3109/1061186X.2012.731068-
dc.identifier.urihttp://repository.unizik.edu.ng/handle/123456789/473-
dc.descriptionScholarly Articleen_US
dc.description.abstractBackground: To fully exploit organic cation transporters for targeted drug delivery in the lung, the use of a readily available and well-characterized tissue culture model and cheap easily detectable substrates is indispensable. Objectives: To investigate the suitability of Calu-3 as tissue model for characterizing organic cation permeation across the bronchial cells using a fmuorescent dye,4(4 (Dimethylamino) styryl)-N-methylpyridinium iodide (4-DI-1-ASP). Methods: Substrate uptake, inhibition, and transport were performed to establish active transport mechanism. Organic cation transporter expression was determined with quantitative polymerase chain reaction (qPCR), immune-histochemistry, and fmuorescent microscopy. Results:4-Di-1-ASP uptake in Calu-3 cells was concentration (Km = 2.7 ± 0.3 mM, V max= 4.6 ± 2.6 nmol/µg protein/30 min), temperature (uptake at 37°C>>4°C), and pH dependent (higher uptake at pH ≥ 7). L-carnitine, verapamil, and corticosterone signifjcantly inhibited its uptake with IC50of 28.2, 0.81, and 0.12 mM, respectively. Transport of the dye across the cells was polarized (AP→BL transport was 2.5-fold > BL→AP), saturable (Km = 43.9 ± 3.2) (µM; Vmax =0.0228± nmol/cm2/sec) and reduced 3-fold by metabolic inhibition. The expression pattern of the organic cation transporters (OCT) and carnitine/organic cation transporter (OCTN) isoforms was: OCT1<<OCT3 <OCTN1<OCTN2; OCT2 was not detected. Conclusions: Based on qPCR, immunohistochemistry, uptake and transport data, the Calu-3 cells can be used as a model for not only studying strategies for optimizing the efgect of inhaled organic cations, but also for cross-validating newly-developed respiratory cell lines.en_US
dc.language.isoenen_US
dc.publisherInformaen_US
dc.subjectPulmonary epitheliumen_US
dc.subjectorganic cation transporters (OCT1-3)en_US
dc.subjectcarnitine/organic cation transporteren_US
dc.titleCharacterization of Calu-3 cell monolayers as a model of bronchial epithelial transport: organic cation interaction studiesen_US
dc.typeArticleen_US
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