Peptide Anchor for Folate-Targeted Liposomal Delivery

Specific folate receptors are abundantly overexpressed in chronically activated macrophages and in most cancer cells. Directed folate receptor targeting using liposomes is usually achieved using folate linked to a phospholipid or cholesterol anchor. This link is formed using a large spacer like poly...

Descripción completa

Detalles Bibliográficos
Autores: Nogueira, Eugénia, Mangialavori, Irene Cecilia, Loureiro, Ana, Azoia, Nuno G., Sárria, Marisa P., Nogueira, Patrícia, Freitas, Jaime, Härmark, Johan, Shimanovich, Ulyana, Rollett, Alexandra, Lacroix, Ghislaine, Bernardes, Gonçalo J.L., Guebitz, Georg, Hebert, Hans, Moreira, Alexandra, Carmo, Alexandre M., Rossi, Juan Pablo Francisco, Gomes, Andreia C., Preto, Ana, Cavaco Paulo, Artur
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2015
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/100056
Acceso en línea:http://hdl.handle.net/11336/100056
Access Level:acceso abierto
Palabra clave:FOLATE RECEPTORS
PEPTIDE CONJUGATE
NANOLIPOSOMES
DROG DELIVERY
https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
Descripción
Sumario:Specific folate receptors are abundantly overexpressed in chronically activated macrophages and in most cancer cells. Directed folate receptor targeting using liposomes is usually achieved using folate linked to a phospholipid or cholesterol anchor. This link is formed using a large spacer like polyethylene glycol. Here, we report an innovative strategy for targeted liposome delivery that uses a hydrophobic fragment of surfactant protein D linked to folate. Our proposed spacer is a small 4 amino acid residue linker. The peptide conjugate inserts deeply into the lipid bilayer without affecting liposomal integrity, with high stability and specificity. To compare the drug delivery potential of both liposomal targeting systems, we encapsulated the nuclear dye Hoechst 34580. The eventual increase in blue fluorescence would only be detectable upon liposome disruption, leading to specific binding of this dye to DNA. Our delivery system was proven to be more efficient (2-fold) in Caco-2 cells than classic systems where the folate moiety is linked to liposomes by polyethylene glycol.

Similares en LA Referencia