Cyclodextrin polymers as carriers for the platinum-based anticancer agent LA-12

Valentina Giglio, Maurizio Viale, Massimiliano Monticone, Angela M. Aura, Giuseppe Spoto, Giovanni Natile, Francesco P. Intini, Graziella Vecchio

Research output: Contribution to journalArticle

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Abstract

Polymeric nanoparticles containing cyclodextrins are currently undergoing clinical trials as nanotherapeutics. In this context, we have synthesized high and low molecular weight β-cyclodextrin polymers and functionalized them with folate to improve their selectivity for cells overexpressing the folic acid receptor. Inclusion complexes of the unfunctionalized and FA-functionalized polymers with the antitumour complex cis-trans-cis-[PtCl2(CH3CO2)2(adamantyl-NH2)(NH3)] (LA-12) have been tested on tumour cells. In the presence of the high molecular weight polymers, LA-12 exhibited IC50 values significantly lower than that of LA-12 alone in MDA-MB-231 cells. The drug nanocarriers investigated do not appear to take significant advantage of the presence of folate residues, possibly because of the reduced accessibility of folate included in cyclodextrin moieties by the receptor or low degree of functionalization of the polymers. However the non-covalent approach, based on inclusion complexes with cyclodextrin polymers, looks very promising for improving the performance of LA-12.

Original languageEnglish
Pages (from-to)12461-12466
Number of pages6
JournalRSC Advances
Volume6
Issue number15
DOIs
Publication statusPublished - 2016

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Cyclodextrins
Platinum
Folic Acid
Antineoplastic Agents
Polymers
Molecular weight
Tumors
Cells
Nanoparticles
cyclodextrin polymer
Pharmaceutical Preparations
Acids

ASJC Scopus subject areas

  • Chemical Engineering(all)
  • Chemistry(all)

Cite this

Giglio, V., Viale, M., Monticone, M., Aura, A. M., Spoto, G., Natile, G., ... Vecchio, G. (2016). Cyclodextrin polymers as carriers for the platinum-based anticancer agent LA-12. RSC Advances, 6(15), 12461-12466. https://doi.org/10.1039/c5ra22398a

Cyclodextrin polymers as carriers for the platinum-based anticancer agent LA-12. / Giglio, Valentina; Viale, Maurizio; Monticone, Massimiliano; Aura, Angela M.; Spoto, Giuseppe; Natile, Giovanni; Intini, Francesco P.; Vecchio, Graziella.

In: RSC Advances, Vol. 6, No. 15, 2016, p. 12461-12466.

Research output: Contribution to journalArticle

Giglio, V, Viale, M, Monticone, M, Aura, AM, Spoto, G, Natile, G, Intini, FP & Vecchio, G 2016, 'Cyclodextrin polymers as carriers for the platinum-based anticancer agent LA-12', RSC Advances, vol. 6, no. 15, pp. 12461-12466. https://doi.org/10.1039/c5ra22398a
Giglio, Valentina ; Viale, Maurizio ; Monticone, Massimiliano ; Aura, Angela M. ; Spoto, Giuseppe ; Natile, Giovanni ; Intini, Francesco P. ; Vecchio, Graziella. / Cyclodextrin polymers as carriers for the platinum-based anticancer agent LA-12. In: RSC Advances. 2016 ; Vol. 6, No. 15. pp. 12461-12466.
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