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Peptide Anchor for Folate-Targeted Liposomal Delivery

2015; American Chemical Society; Volume: 16; Issue: 9 Linguagem: Inglês

10.1021/acs.biomac.5b00823

1526-4602

Eugénia Nogueira, Irene C. Mangialavori, Ana Loureiro, Nuno G. Azóia, Marisa P. Sárria, Patrícia Nogueira, Jaime Freitas, Johan Härmark, Ulyana Shimanovich, Alexandra Rollett, Ghislaine Lacroix, Gonçalo J. L. Bernardes, Georg M. Guebitz, Hans Hebert, Alexandra Moreira, Alexandre M. Carmo, Juan Pablo F.C. Rossi, Andreia C. Gomes, Ana Preto, Artur Cavaco‐Paulo,

Advanced biosensing and bioanalysis techniques

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.