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Sucrose Esters Increase Drug Penetration, But Do Not Inhibit P‐Glycoprotein in Caco‐2 Intestinal Epithelial Cells

Kiss, Lóránd ; Hellinger, Éva ; Pilbat, Ana‐Maria ; Kittel, Ágnes ; Török, Zsolt ; Füredi, András ; Szakács, Gergely ; Veszelka, Szilvia ; Sipos, Péter ; Ózsvári, Béla ; Puskás, László G. ; Vastag, Monika ; Szabó‐Révész, Piroska ; Deli, Mária A.

Journal of pharmaceutical sciences, 2014-10, Vol.103 (10), p.3107-3119 [Periódico revisado por pares]

United States: Elsevier Inc

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Título:
Sucrose Esters Increase Drug Penetration, But Do Not Inhibit P‐Glycoprotein in Caco‐2 Intestinal Epithelial Cells
Autor: Kiss, Lóránd ; Hellinger, Éva ; Pilbat, Ana‐Maria ; Kittel, Ágnes ; Török, Zsolt ; Füredi, András ; Szakács, Gergely ; Veszelka, Szilvia ; Sipos, Péter ; Ózsvári, Béla ; Puskás, László G. ; Vastag, Monika ; Szabó‐Révész, Piroska ; Deli, Mária A.
Assuntos: absorption enhancer ; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism ; Caco-2 Cells ; Chromatography, High Pressure Liquid ; drug permeability ; efflux pumps ; epithelial ; Esters - chemistry ; Humans ; Intestinal Mucosa - drug effects ; Intestinal Mucosa - metabolism ; membrane fluidity ; Membrane Fluidity - drug effects ; P‐glycoprotein ; Sucrose - chemistry ; Sucrose - pharmacology ; sucrose ester ; tight junction ; toxicity
É parte de: Journal of pharmaceutical sciences, 2014-10, Vol.103 (10), p.3107-3119
Descrição: Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water‐soluble sucrose esters, palmitate (P‐1695), myristate (M‐1695), laurate (D‐1216), and two reference absorption enhancers, Tween 80 and Cremophor RH40, were tested on Caco‐2 cells. Caco‐2 monolayers formed a good barrier as reflected by high transepithelial resistance and positive immunostaining for junctional proteins claudin‐1, ZO‐1, and β‐catenin. Sucrose esters in nontoxic concentrations significantly reduced resistance and impedance, and increased permeability for atenolol, fluorescein, vinblastine, and rhodamine 123 in Caco‐2 monolayers. No visible opening of the tight junctions was induced by sucrose esters assessed by immunohistochemistry and electron microscopy, but some alterations were seen in the structure of filamentous actin microfilaments. Sucrose esters fluidized the plasma membrane and enhanced the accumulation of efflux transporter ligands rhodamine 123 and calcein AM in epithelial cells, but did not inhibit the P‐glycoprotein (P‐gp)‐mediated calcein AM accumulation in MES‐SA/Dx5 cell line. These data indicate that in addition to their dissolution‐increasing properties sucrose esters can enhance drug permeability through both the transcellular and paracellular routes without inhibiting P‐gp. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:3107–3119, 2014
Editor: United States: Elsevier Inc
Idioma: Inglês

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Sucrose Esters Increase Drug Penetration, But Do Not Inhibit P‐Glycoprotein in Caco‐2 Intestinal Epithelial Cells

Kiss, Lóránd ; Hellinger, Éva ; Pilbat, Ana‐Maria ; Kittel, Ágnes ; Török, Zsolt ; Füredi, András ; Szakács, Gergely ; Veszelka, Szilvia ; Sipos, Péter ; Ózsvári, Béla ; Puskás, László G. ; Vastag, Monika ; Szabó‐Révész, Piroska ; Deli, Mária A.

United States: Elsevier Inc

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