In vitro intestinal co-culture cell model to evaluate intestinal absorption of edelfosine lipid nanoparticles

Nanotechnology is providing a new therapeutic paradigm by enhancing drug efficacy and preventing side-effects. Edelfosine is a synthetic ether lipid analogue of platelet activating factor with high antitumor activity. The encapsulation of this potent antitumor drug in lipid nanoparticles increases i...

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Detalles Bibliográficos
Autores: Blanco-Prieto, M.J. (María José)|||/items/93e177db-635f-456f-b672-b79ef8befc40, Sebastian, V. (Víctor)|||/items/42de1b00-b9b3-4844-830d-2c795578a861, Guada, M. (Melissa)|||/items/e6d8d28f-a4ea-4292-a09c-5bad78e34564, Lasa-Saracibar, B. (Beatriz)|||/items/01d03220-3bc2-4e01-8b38-247a935720cd
Tipo de recurso: artículo
Fecha de publicación:2014
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/36747
Acceso en línea:https://hdl.handle.net/10171/36747
Access Level:acceso abierto
Palabra clave:Transport
Raji
Permeabiltity
Lipid nanoparticles
Edelfosine
Caco-2
Descripción
Sumario:Nanotechnology is providing a new therapeutic paradigm by enhancing drug efficacy and preventing side-effects. Edelfosine is a synthetic ether lipid analogue of platelet activating factor with high antitumor activity. The encapsulation of this potent antitumor drug in lipid nanoparticles increases its oral bioavailability; moreover, it prevents the hemolytic and gastrointestinal side-effects of the free drug. The literature points towards lymphatic absorption of lipid nanoparticles after oral administration, and previous in vitro and in vivo studies stress the protection against toxicity that these nanosystems provide. The present study is intended to assess the permeability of lipid nanoparticles across the intestinal barrier. Caco-2 monoculture and Caco-2/Raji co-culture were used as in vitro models of enterocytes and Microfold cells respectively. Results showed that free drug is internalized and possibly metabolized in enterocytes. These results do not correlate with those observed in vivo when edelfosine-lipid nanoparticles were administered orally in mice, which suggests that the microfold model is not a good model to study the absorption of edelfosine-lipid nanoparticles across the intestinal barrier in vitro.