Peptide Anchor for Folate-Targeted Liposomal Delivery
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- 作者：Eug茅nia Nogueira ; Irene C. Mangialavori ; Ana Loureiro ; Nuno G. Azoia ; Marisa P. S谩rria ; Patr铆cia Nogueira ; Jaime Freitas ; Johan H盲rmark ; Ulyana Shimanovich ; Alexandra Rollett ; Ghislaine Lacroix ; Gon莽alo J. L. Bernardes ; Georg Guebitz ; Hans Hebert ; Alexandra Moreira ; Alexandre M. Carmo ; Juan Pablo F. C. Rossi ; Andreia C. Gomes ; Ana Preto ; Artur Cavaco-Paulo
- 刊名：Biomacromolecules
- 出版年：2015
- 出版时间：September 14, 2015
- 年：2015
- 卷：16
- 期：9
- 页码：2904-2910
- 全文大小：347K
- ISSN：1526-4602
文摘
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.