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Issue 43, 2016
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Functionalized nonporous silica nanoparticles as carriers for Pt(IV) anticancer prodrugs

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Nonporous silica nanoparticles (SNPs) with an external shell containing primary amino groups were proposed as potential delivery systems for Pt(IV) antitumor prodrugs. Spherical SNPs containing two different external arms, i.e. 3-aminopropyl and N-(6-aminohexyl)aminomethylene, of around 125 nm hydrodynamic diameter were loaded with two different cisplatin-based Pt(IV) complexes, namely (OC-6-44)-diamminedichloridoethoxidosuccinatoplatinum(IV) and (OC-6-44)-diamminedichloridoacetylamidosuccinatoplatinum(IV), through the formation of amide bonds between the pendant amino groups on SNPs and the free carboxylic group of the complexes. In the presence of the N-(6-aminohexyl)aminomethylene arm, the Pt(IV)–SNP conjugates showed a negligible (unwanted) Pt release by hydrolysis, whereas in the presence of ascorbic acid the reduction of Pt(IV) → Pt(II) caused the substantial release of the active metabolite cisplatin. Conjugate Pt(IV)–SNP exhibited better antiproliferative activity on the Pt-sensitive A2780 human ovarian cancer cell line than the parent cisplatin and their free Pt(IV) precursors, due to their more efficient cellular uptake, likely by endocytosis.

Graphical abstract: Functionalized nonporous silica nanoparticles as carriers for Pt(iv) anticancer prodrugs

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Publication details

The article was received on 06 Aug 2016, accepted on 22 Sep 2016 and first published on 23 Sep 2016

Article type: Paper
DOI: 10.1039/C6DT03133A
Citation: Dalton Trans., 2016,45, 17233-17240
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    Functionalized nonporous silica nanoparticles as carriers for Pt(IV) anticancer prodrugs

    M. Ravera, E. Gabano, I. Zanellato, E. Perin, A. Arrais and D. Osella, Dalton Trans., 2016, 45, 17233
    DOI: 10.1039/C6DT03133A

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