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EnglishSupramolecular 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, flowcytometry analysis and b-scintillation highlighted that FT-SVAswere 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. SVAswere accumulated mainly in the lungs, spleen and kidneys, while FT-SVAswere 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.
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. BIOMATERIALS, 31, 7340-7354.
| Data di pubblicazione: | 2010 |
| Titolo: | FOLATE-TARGETED SUPRAMOLECULAR VESICULAR AGGREGATES BASED ON POLYASPARTYL-HYDRAZIDE COPOLYMERS FOR THE SELECTIVE DELIVERY OF ANTITUMORAL DRUGS |
| Autori: | |
| Citazione: | 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. BIOMATERIALS, 31, 7340-7354. |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.10016/J.biomaterials 2010.05.060 |
| 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, flowcytometry analysis and b-scintillation highlighted that FT-SVAswere 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. SVAswere accumulated mainly in the lungs, spleen and kidneys, while FT-SVAswere 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. |
| Settore Scientifico Disciplinare: | Settore CHIM/09 - Farmaceutico Tecnologico Applicativo |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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