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Peptide Anchor for Folate-Targeted Liposomal Delivery

Eugenia Nogueira Irene C. Mangialavori Ana Loureiro Nuno G. Azoia Marisa P. Saarria Patricia Nogueira Jaime Freitas Johan Harmark Ulyana Shimanovich Alexandra Rollett 1 Ghislaine Lacroix 2 Goncalo J.L. Bernardes Georg Guebitz 1 Hans Hebert Alexandra Moreira Alexandre M. Carmo Juan Pablo Rossi Andreia C. Gomes Ana Preto Artur Cavaco-Paulo
1 BOKU - Universität für Bodenkultur Wien = University of Natural Resources and Life [Vienne, Autriche]
2 INERIS - Institut National de l'Environnement Industriel et des Risques
Abstract : 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.
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Submitted on : Tuesday, August 7, 2018 - 2:24:45 PM
Last modification on : Thursday, March 31, 2022 - 1:00:20 PM

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Eugenia Nogueira, Irene C. Mangialavori, Ana Loureiro, Nuno G. Azoia, Marisa P. Saarria, et al.. Peptide Anchor for Folate-Targeted Liposomal Delivery. Biomacromolecules, American Chemical Society, 2015, 16 (9), pp.2904-2910. ⟨10.1021/acs.biomac.5b00823⟩. ⟨ineris-01855132⟩

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