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TitlePeptide anchor for folate-targeted liposomal delivery
Author(s)Nogueira, E.
Mangialavori, Irene C.
Loureiro, Ana
Azóia, Nuno G.
Sarria, Marisa P.
Nogueira, Patrícia
Freitas, Jaime
Harmark, Johan
Shimanovich, Ulyana
Rollett, Alexandra
Lacroix, Ghislaine
Bernardes, Gonçalo J. L.
Guebitz, Georg
Hebert, Hans
Moreira, Alexandra
Carmo, Alexandre M.
Rossi, Juan Pablo F. C.
Gomes, Andreia
Preto, Ana
Cavaco-Paulo, Artur
Issue date4-Aug-2015
PublisherACS Publications
CitationNogueira, E.; Irene C. Mangialavori; Loureiro, A.; Azoia, Nuno G.; Passos, M.; Patrícia Nogueira; Jaime Freitas; Harmark, J.; Ulyana Shimanovich; Ulyana Shimanovich; Alexandra Rollett; Ghislaine Lacroix; Bernardes, Gonçalo J. L.; Guebitz, Georg; Hebert, H.; Alexandra Moreira; Alexandre M. Carmo; Juan Pablo F. C. Rossi; Andreia Gomes; Ana Preto; Paulo, Artur Cavaco, Peptide anchor for folate-targeted liposomal delivery. Biomacromolecules, 16(9), 2904-2910, 2015
Abstract(s)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.
Publisher version
AccessOpen access
Appears in Collections:CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series
DBio - Artigos/Papers

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