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Pregled bibliografske jedinice broj: 513761

Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays


Nožinić, Danijela; Milić, Astrid; Mikac, Lara; Ralić, Jovica; Padovan, Jasna; Antolović, Roberto
Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays // Croatica chemica acta, 83 (2010), 323-331 (međunarodna recenzija, članak, znanstveni)


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Naslov
Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays

Autori
Nožinić, Danijela ; Milić, Astrid ; Mikac, Lara ; Ralić, Jovica ; Padovan, Jasna ; Antolović, Roberto

Izvornik
Croatica chemica acta (0011-1643) 83 (2010); 323-331

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
macrolides; permeability; P-glycoprotein; PAMPA; Caco-2; MDCK

Sažetak
The transport of commercially available macrolide antibiotics erythromycin, clarithromycin, roxithromycin, azithromycin, and telithromycin was studied by PAMPA, a model of passive diffusion, and by two models of active transport, Caco-2 and MDCKII-hMDR1. An involvement of efflux pump P-glycoprotein (P-gp) in macrolide transport was also examined. Generally, in Caco-2 and MDCKII-hMDR1 assays without P-gp inhibition, a significantly lower apparent permeability (Papp) in apical-to-basolateral (AB) than basolateral-to-apical (BA) direction was observed [efflux ratio, Pappratio(BA/AB) > 4.2]. Upon P-gp inhibition, Papp(AB) was increased and Papp(BA) was decreased. The observed Papp values, their efflux ratios, as well as a significant decrease in efflux ratios caused by P-gp inhibition (> 50 %) qualify all tested macrolides as P-gp substrates. Results obtained with PAMPA suggest that this assay is not a method of choice for screening of macrolide permeability due to the lack of P-gp efflux pump and/or other transporters potentially involved in macrolide transport.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija



POVEZANOST RADA


Ustanove:
Sveučilište u Rijeci - Odjel za biotehnologiju

Profili:

Avatar Url Jovica Ralić (autor)

Avatar Url Astrid Milić (autor)

Avatar Url Roberto Antolović (autor)

Avatar Url Jasna Padovan (autor)

Avatar Url Lara Mikac (autor)

Citiraj ovu publikaciju

Nožinić, Danijela; Milić, Astrid; Mikac, Lara; Ralić, Jovica; Padovan, Jasna; Antolović, Roberto
Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays // Croatica chemica acta, 83 (2010), 323-331 (međunarodna recenzija, članak, znanstveni)
Nožinić, D., Milić, A., Mikac, L., Ralić, J., Padovan, J. & Antolović, R. (2010) Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays. Croatica chemica acta, 83, 323-331.
@article{article, year = {2010}, pages = {323-331}, keywords = {macrolides, permeability, P-glycoprotein, PAMPA, Caco-2, MDCK}, journal = {Croatica chemica acta}, volume = {83}, issn = {0011-1643}, title = {Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays}, keyword = {macrolides, permeability, P-glycoprotein, PAMPA, Caco-2, MDCK} }
@article{article, year = {2010}, pages = {323-331}, keywords = {macrolides, permeability, P-glycoprotein, PAMPA, Caco-2, MDCK}, journal = {Croatica chemica acta}, volume = {83}, issn = {0011-1643}, title = {Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays}, keyword = {macrolides, permeability, P-glycoprotein, PAMPA, Caco-2, MDCK} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus





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