Complete Inhibition of Extranodal Dissemination of Lymphoma by Edelfosine-Loaded Lipid Nanoparticles

Autores: Estella Hermoso de Mendoza, Ander; Campanero Martínez, Miguel Ángel; Lana Vega, Hugo; Villa-Pulgarin, J. A.; De La Iglesia-Vicente, J.; Mollinedo, F.; Blanco Prieto, María José
Título de la revista: NANOMEDICINE
ISSN: 1743-5889
Volumen: 7
Número: 5
Páginas: 679 - 690
Fecha de publicación: 2012
Lugar: WOS
Background: Lipid nanoparticles (LNs) made of synthetic lipids Compritol (R) 888 ATO and Precirol (R) ATO 5 were developed with an average size of 110.4 +/- 2.1 and 103.1 +/- 2.9 nm, and an encapsulation efficiency above 85% for both type of lipids. These LNs decrease the hemolytic toxicity of the drug by 90%. Materials & methods: Pharmacokinetic and biodistribution profiles of the drug were studied after intravenous and oral administration of edelfosine-containing LNs. Results: This provided an increase in relative oral bioavailability of 1500% after a single oral administration of drug-loaded LNs, maintaining edelfosine plasma levels over 7 days in contrast to a single oral administration of edelfosine solution, which presented a relative oral bioavailability of 10%. Moreover, edelfosine-loaded LNs showed a high accumulation of the drug in lymph nodes and resulted in slower tumor growth than the free drug in a murine lymphoma xenograft model, as well as potent extranodal dissemination inhibition.