http://www.cnr.it/ontology/cnr/individuo/prodotto/ID9795
Folate-Targeted supramolecular vesicular aggregates based on polyaspartyl hydrazide copolymers for the selective delivery of antitumoral drugs. (Articolo in rivista)
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- Label
- Folate-Targeted supramolecular vesicular aggregates based on polyaspartyl hydrazide copolymers for the selective delivery of antitumoral drugs. (Articolo in rivista) (literal)
- Anno
- 2010-01-01T00:00:00+01:00 (literal)
- Alternative label
Licciardi M., Paolino D., Celia C., Giammona G., Cavallaro G., Fresta M. (2010)
Folate-Targeted supramolecular vesicular aggregates based on polyaspartyl hydrazide copolymers for the selective delivery of antitumoral drugs.
in Biomaterials
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Licciardi M., Paolino D., Celia C., Giammona G., Cavallaro G., Fresta M. (literal)
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- ISI Web of Science (WOS) (literal)
- Titolo
- Folate-Targeted supramolecular vesicular aggregates based on polyaspartyl hydrazide copolymers for the selective delivery of antitumoral drugs. (literal)
- Abstract
- Supramolecular vesicular aggregates (SVAs) have the advantage of combining the safe and biocompatible properties of colloidal vesicular carriers based on phospholipids with those of polymeric materials, i.e. polyaspartyl-hydrazide (PAHy) copolymers. To provide SVAs with a certain tumour selectivity, folate moieties were chemically conjugated to PAHy copolymers. Physicochemical properties (mean sizes, polydispersity index and zeta potential) of folate-targeted SVAs (FT-SVAs) loaded with gemcitabine were evaluated. The antiproliferative and anticancer activity of gemcitabine-loaded FT-SVAs was evaluated against two cancer cell lines, i.e. MCF-7 cells which over-express the folate receptor and the BxPC-3 cells, which do not over-express this receptor. Gemcitabine-loaded FT-SVAs showed a significantly (p < 0.001) greater and more specific in vitro anticancer activity with respect to both the free drug and the drug-loaded conventional liposomes or untargeted SVAs. Confocal microscopy, flow cytometry analysis and beta-scintillation highlighted that FT-SVAs were able to interact with MCF-7 cells after just 3 h and to increase the amount internalization in cells over-expressing the folate receptor. The in vivo biodistribution and pharmacokinetic experiments showed that gemcitabine-loaded SVAs and FT-SVAs were removed from the circulatory system at a slower rate than the native drug and a prolonged gemcitabine plasma concentration was observed for up to 16 h. SVAs were accumulated mainly in the lungs, spleen and kidneys, while FT-SVAs were also up taken by brain. These interesting and stimulating results suggest the existence of a possible in vivo application of SVAs and encourage the use of folate as a targeting agent in anticancer therapy. (literal)
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