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Journal Articles Biomacromolecules Year : 2015

Peptide Anchor for Folate-Targeted Liposomal Delivery

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Eugenia Nogueira
  • Function : Author
Irene C. Mangialavori
  • Function : Author
Ana Loureiro
  • Function : Author
Nuno G. Azoia
  • Function : Author
Marisa P. Saarria
  • Function : Author
Patricia Nogueira
  • Function : Author
Jaime Freitas
  • Function : Author
Johan Harmark
  • Function : Author
Ulyana Shimanovich
  • Function : Author
Goncalo J.L. Bernardes
  • Function : Author
Hans Hebert
  • Function : Author
Alexandra Moreira
  • Function : Author
Alexandre M. Carmo
  • Function : Author
Juan Pablo Rossi
  • Function : Author
Andreia C. Gomes
  • Function : Author
Ana Preto
  • Function : Author
Artur Cavaco-Paulo
  • Function : Author

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.

Dates and versions

ineris-01855132 , version 1 (07-08-2018)

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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, 2015, 16 (9), pp.2904-2910. ⟨10.1021/acs.biomac.5b00823⟩. ⟨ineris-01855132⟩

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