Lipid nanoparticles protect from edelfosine toxicity in vivo.
Int J Pharm
; 474(1-2): 1-5, 2014 Oct 20.
Article
em En
| MEDLINE
| ID: mdl-25091376
ABSTRACT
Edelfosine, an alkyl-lysophospholipid antitumor drug with severe side-effects, has previously been encapsulated into lipid nanoparticles (LN) with the purpose of improving their toxicity profile. LN are made of lipids recognized as safe by the Food and Drug Administration (FDA) and, therefore, these systems are generally considered as nontoxic vehicles. However, toxicity studies regarding the use of LN as vehicles for drug administration are limited. In the present study, we investigated the in vivo toxicity of free edelfosine, and the protection conferred by LN. The free drug, non-loaded LN and edelfosine-loaded LN were orally administered to mice. Our results show that the oral administration of the free drug at 4 times higher than the therapeutic dose caused the death of the animals within 72h. Moreover, histopathology revealed gastrointestinal toxicity and an immunosuppressive effect. In contrast, LN showed a protective effect against edelfosine toxicity even at the higher dose and were completely safe. LN are, therefore, a safe vehicle for the administration of edelfosine by the oral route. The nanosystems developed could be further used for the administration of other drugs.
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Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Éteres Fosfolipídicos
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Nanopartículas
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Gastroenteropatias
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Lipídeos
Limite:
Animals
Idioma:
En
Revista:
Int J Pharm
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Espanha