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Molecules 2016, 21(4), 522; doi:10.3390/molecules21040522

Delivery of Gemcitabine Prodrugs Employing Mesoporous Silica Nanoparticles

1
Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Via P. Giuria 9, 10125 Torino, Italy
2
Dipartimento di Chimica and NIS (Nanostructured Interfaces and Surfaces) Centre, Università di Torino, Via P. Giuria 7, 10125 Torino, Italy
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 21 March 2016 / Revised: 13 April 2016 / Accepted: 14 April 2016 / Published: 21 April 2016
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Abstract

In this paper, mesoporous silica nanoparticles (MSNs) were studied as vehicles for the delivery of the antitumoral drug gemcitabine (GEM) and of its 4-(N)-acyl derivatives, (4-(N)-valeroyl-(C5GEM), 4-(N)-lauroyl-(C12GEM) and 4-(N)-stearoyl-gemcitabine (C18GEM)). The loading of the GEM lipophilic prodrugs on MSNs was explored with the aim to obtain both a physical and a chemical protection of GEM from rapid plasmatic metabolization. For this purpose, MSNs as such or with grafted aminopropyl and carboxyethyl groups were prepared and characterized. Then, their different drug loading capacity in relation to the nature of the functional group was evaluated. In our experimental conditions, GEM was not loaded in any MSNs, while C12GEM was the most efficiently encapsulated and employed for further evaluation. The results showed that loading capacity increased with the presence of functional groups on the nanoparticles; similarly, the presence of functional groups on MSNs’ surface influenced the drug release profile. Finally, the cytotoxicity of the different preparations was evaluated and data showed that C12GEM loaded MSNs are less cytotoxic than the free drug with an activity that increased with the incubating time, indicating that all these systems are able to release the drug in a controlled manner. Altogether, the results demonstrate that these MSNs could be an interesting system for the delivery of anticancer drugs. View Full-Text
Keywords: mesoporous silica nanoparticles; drug delivery systems; anticancer drugs; prodrugs; biomaterials; surface chemistry mesoporous silica nanoparticles; drug delivery systems; anticancer drugs; prodrugs; biomaterials; surface chemistry
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Malfanti, A.; Miletto, I.; Bottinelli, E.; Zonari, D.; Blandino, G.; Berlier, G.; Arpicco, S. Delivery of Gemcitabine Prodrugs Employing Mesoporous Silica Nanoparticles. Molecules 2016, 21, 522.

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