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.
journal_name
Biomacromoleculesjournal_title
Biomacromoleculesauthors
Nogueira E,Mangialavori IC,Loureiro A,Azoia NG,Sárria MP,Nogueira P,Freitas J,Härmark J,Shimanovich U,Rollett A,Lacroix G,Bernardes GJ,Guebitz G,Hebert H,Moreira A,Carmo AM,Rossi JP,Gomes AC,Preto A,Cavaco-Paulo Adoi
10.1021/acs.biomac.5b00823subject
Has Abstractpub_date
2015-09-14 00:00:00pages
2904-10issue
9eissn
1525-7797issn
1526-4602journal_volume
16pub_type
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