AutoriAntonino Mazzaglia+ Maria Luisa Bondì, Angela Scala, Francesca Zito,Giovanna Barbieri, Francesco Crea, Giuseppina Vianelli, Placido G. Mineo,Tiziana Fiore, Claudia Pellerito, Lorenzo Pellerito, and Maria Assunta Costa.
AbstractAmphiphilic cyclodextrin (ACyD) provides watersolubleand adaptable nanovectors by modulating the balancebetween the hydrophobic and hydrophilic chains at both CyDsides. This work aimed to design nanoassemblies based onnonionic and hydrophilic ACyD (SC6OH) for the delivery of apoor-water-soluble organotin(IV)-porphyrin derivative[(Bu3Sn)4TPPS] to melanoma cancer cells. To characterize theporphyrin derivatives under simulated physiological conditions, aspeciation was performed using complementary techniques. Inaqueous solution (<=20 ?M), (Bu3Sn)4TPPS primarily exists as amonomer (2 in Figure 1), as suggested by the low staticanisotropy (? ? 0.02) with a negligible formation of porphyrinsupramolecular aggregates. MALDI-TOF spectra indicate thepresence of moieties (i.e., [(Bu3Sn)3TPPS]-) that are derivatives of the monomeric species. Spectrofluorimetry coupled withpotentiometric measurements primarily assesses the presence of the hydrolytic [(Bu3Sn)4TPPS (OH)4]4- species underphysiological conditions. Nanoassemblies of (Bu3Sn)4TPPS/SC6OH were prepared by dispersion of organic films in PBS at pH7.4 and were investigated using a combination of spectroscopic and morphological techniques. The UV-vis and emissionfluorescence spectra of the (Bu3Sn)4TPPS/SC6OH reveal shifts in the peculiar bands of the organotin(IV)-porphyrin derivativedue to its interaction with the ACyD supramolecular assemblies in aqueous solution. The mean size was within the range of100-120 nm. The ?-potential was negative (-16 mV) for the (Bu3Sn)4TPPS/SC6OH nanoassemblies, with an entrapmentefficiency of approximately 67%. The intracellular delivery, cytotoxicity, nuclear morphology and cell growth kinetics wereevaluated via fluorescence microscopy on A375 human melanoma cells. The delivery of (Bu3Sn)4TPPS by ACyD with respect tofree (Bu3Sn)4TPPS increases the internalization efficiency and cytotoxicity to induce apoptotic cell death and, at lowerconcentrations, changes the cellular morphology and prevents cell proliferation.
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Pagina inizio3820
Pagina fine3829
Autori IBFMaria Assunta COSTA
Linee di Ricerca IBFMD.P01.002.001