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Peptide Anchor for Folate-Targeted Liposomal Delivery

Nogueira, Eugenia (author)
Mangialavori, Irene C. (author)
Loureiro, Ana (author)
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Azoia, Nuno G. (author)
Sarria, Marisa P. (author)
Nogueira, Patricia (author)
Freitas, Jaime (author)
Härmark, Johan (author)
Karolinska Institutet,KTH,Strukturell bioteknik,Karolinska Inst, Sch Technol & Hlth
Shimanovich, Ulyana (author)
Rollett, Alexandra (author)
Lacroix, Ghislaine (author)
Bernardes, Goncalo J. L. (author)
Guebitz, Georg (author)
Hebert, Hans (author)
Karolinska Institutet
Moreira, Alexandra (author)
Carmo, Alexandre M. (author)
Rossi, Juan Pablo F. C. (author)
Gomes, Andreia C. (author)
Preto, Ana (author)
Cavaco-Paulo, Artur (author)
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 (creator_code:org_t)
2015-08-11
2015
English.
In: Biomacromolecules. - : American Chemical Society (ACS). - 1525-7797 .- 1526-4602. ; 16:9, s. 2904-2910
  • Journal article (peer-reviewed)
Abstract Subject headings
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  • 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.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
NATURVETENSKAP  -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
NATURAL SCIENCES  -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
NATURVETENSKAP  -- Biologi -- Cellbiologi (hsv//swe)
NATURAL SCIENCES  -- Biological Sciences -- Cell Biology (hsv//eng)

Keyword

Surfactant Protein-D
Cyclooxygenase-2 Inhibitor
Inflammatory Response
Carbon-Monoxide
In-Vitro
Celecoxib
Cancer
Cells
Methotrexate
Mechanisms

Publication and Content Type

ref (subject category)
art (subject category)

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