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Artículo

Inhibition of P-glycoprotein pumps by PEO–PPO amphiphiles: branched versus linear derivatives

Alvarez Lorenzo, Carmen; Rey Rico, Ana; Brea, José; Loza, Maria Isabel; Concheiro, Ángel; Sosnik, Alejandro DarioIcon
Fecha de publicación: 12/2010
Editorial: Future Medicine
Revista: Nanomedicine
ISSN: 1743-5889
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Otras Nanotecnología

Resumen

Inhibition of the activity of efflux transporters may relevantly improve the chemotherapy of cancer and infectious diseases. Aim: To explore the ability of poloxamines (Tetronic®, X-shaped structure with a central ethylendiamine group and four branches of poly[ethylene oxide]–poly[propylene oxide] [PEO–PPO]) to inhibit the activity of P-glycoprotein (P-gp) on Caco-2 cell monolayers and to elucidate the incidence of the molecular architecture of PEO–PPO block copolymers on the intracellular accumulation of a relevant substrate, doxorubicin, by comparison with poloxamers (Pluronic®, linear triblock copolymers), well-known inhibitors of this efflux transporter. Methods: Both pristine and N-methylated poloxamines displaying a wide range of molecular weights and EO/PO ratios were tested regarding cytocompatibility and accumulation of doxorubicin in Caco-2 monolayers. Verapamil was used as a control. Results: The most active anti-P-gp poloxamines (which enhanced two- to three-fold doxorubicin accumulation compared with verapamil) resulted to be pristine medium-to-high hydrophobic T304, T904, T1301, T901 and T150R1. A notable dependence of the anti-P-gp activity on the copolymer concentration was found. A joint diagram of the inhibitory activity of poloxamers and poloxamines as a function of the effective length of the PPO block is proposed. Conclusion: The anti-P-gp activity is maxima for block copolymers possessing a low-to-medium hydrophilic–lipophilic balance and an ‘effective number’ of PO units ranging from 30 to 50.
Palabras clave: Cancer , Doxorubicin , Drug Efflux , P-Glycoprotein Inhibition , Poloxamer , Poloxamine , Polymeric Micelle , Transport
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/14453
URL: http://www.futuremedicine.com/doi/full/10.2217/nnm.10.53
DOI: http://dx.doi.org/10.2217/nnm.10.53
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Articulos(OCA HOUSSAY)
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Citación
Alvarez Lorenzo, Carmen; Rey Rico, Ana; Brea, José; Loza, Maria Isabel; Concheiro, Ángel; et al.; Inhibition of P-glycoprotein pumps by PEO–PPO amphiphiles: branched versus linear derivatives; Future Medicine; Nanomedicine; 5; 9; 12-2010; 1371-1383
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