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Effects of polyethylene glycols on intestinal efflux pump expression and activity in Caco-2 cells
Hodaei, Darya; Baradaran, Behzad; Valizadeh, Hadi; Zakeri-Milani, Parvin.
  • Hodaei, Darya; Tabriz University of Medical Sciences. Faculty of Pharmacy. Tabriz. IR
  • Baradaran, Behzad; Tabriz University of Medical Sciences. Faculty of Pharmacy. Tabriz. IR
  • Valizadeh, Hadi; Tabriz University of Medical Sciences. Faculty of Pharmacy. Tabriz. IR
  • Zakeri-Milani, Parvin; Tabriz University of Medical Sciences. Faculty of Pharmacy. Tabriz. IR
Braz. j. pharm. sci ; 51(3): 745-753, July-Sept. 2015. graf
Article in English | LILACS | ID: lil-766324
Responsible library: BR1.1
ABSTRACT
The present study was planned to investigate the influence of polyethylene glycols (PEGs) on the activity and expression of P-glycoprotein (P-gp). Sub-toxic concentrations of PEGs in Caco-2 cells were determined using the MTT test assay. Then the measurement of Rhodamine-123 (Rho-123) uptake, a P-gp fluorescence substrate, in Caco-2 cells confronting PEG 400 (1% and 2% w/v), PEG 4000 (2% and 4% w/v), PEG 6000 (2% and 4% w/v), PEG 10000 (2% and 4% w/v), PEG 15000 (1% and 2% w/v), and PEG 35000 (2% and 4% w/v) overnight was taken to elucidate whether non-toxic concentrations of PEGs are able to impact P-gp activity. Furthermore, western blotting was carried out to investigate P-gp protein expression. The results showed that PEG 400 at concentrations of 1% (w/v) and 2% (w/v) and PEG 6000 at the concentration of 4% (w/v) are notably capable of blocking P-gp. Based on the obtained results it is concluded that the mentioned excipients could be used to obstruct P-gp efflux transporter in order to increase the bioavailability of co-administered substrate drug.
RESUMO
O presente estudo foi planejado para investigar a influência de polietileno glicóis sobre a atividade e expressão da P- glicoproteína (P-gp) . Concentrações sub-tóxicas de PGPs e em células Caco-2 foram determinadas por meio do ensaio de MTT. Em seguida, efetuou-se a a medida de captura de Rodamina-123 (Rho-123), um substrato fluorescente de P-gp, em células Caco-2, confrontando com PEG 400 (1% e 2% m/v), PEG 4000 (2% e 4% m/v) e PEG 6000 (2% e 4% m /v), PEG 10000 (2% e 4% w/v), PEG 15000 (1% e 2% m/v), e PEG 35000 (2% e 4% m/v). Essa medida foi efetuada durante a noite, para saber se as concentrações não tóxicas de excipientes são capazes de influenciar a actividade da P-gp. Além disso, realizou-se o western blotting para investigar a expressão da proteína P-gp. Os resultados mostraram que o PEG 400, nas concentrações de 1% (m/v) e 2% (m/v), e PEG 6000, na concentração de 4% (m/v) são capazes de bloquear P-gp. Com base nos resultados conclui-se que os excipientes mencionados poderiam ser utilizados para obstruir o efluxo por P-gp, a fim de aumentar a biodisponibilidade de do fármaco co-administrado.
Subject(s)


Full text: Available Index: LILACS (Americas) Main subject: Polyethylene Glycols / ATP Binding Cassette Transporter, Subfamily B, Member 1 / Caco-2 Cells Language: English Journal: Braz. j. pharm. sci Year: 2015 Type: Article Affiliation country: Iran Institution/Affiliation country: Tabriz University of Medical Sciences/IR

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Full text: Available Index: LILACS (Americas) Main subject: Polyethylene Glycols / ATP Binding Cassette Transporter, Subfamily B, Member 1 / Caco-2 Cells Language: English Journal: Braz. j. pharm. sci Year: 2015 Type: Article Affiliation country: Iran Institution/Affiliation country: Tabriz University of Medical Sciences/IR