Next Article in Journal
Sulforaphane Analogues with Heterocyclic Moieties: Syntheses and Inhibitory Activities against Cancer Cell Lines
Next Article in Special Issue
Novel N-Substituted 2-(2-(Adamantan-1-yl)-1H-Indol-3-yl)-2-Oxoacetamide Derivatives: Synthesis and Biological Evaluation
Previous Article in Journal
Natural Phytochemicals in the Treatment and Prevention of Dementia: An Overview
Previous Article in Special Issue
Synthesis and Antitumor Evaluation of Novel 5-Hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one Derivatives
Article

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
Molecules 2016, 21(4), 522; https://doi.org/10.3390/molecules21040522
Received: 21 March 2016 / Revised: 13 April 2016 / Accepted: 14 April 2016 / Published: 21 April 2016
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
Show Figures

Graphical abstract

MDPI and ACS Style

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. https://doi.org/10.3390/molecules21040522

AMA Style

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(4):522. https://doi.org/10.3390/molecules21040522

Chicago/Turabian Style

Malfanti, Alessio, Ivana Miletto, Emanuela Bottinelli, Daniele Zonari, Giulia Blandino, Gloria Berlier, and Silvia Arpicco. 2016. "Delivery of Gemcitabine Prodrugs Employing Mesoporous Silica Nanoparticles" Molecules 21, no. 4: 522. https://doi.org/10.3390/molecules21040522

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop