Solid lipid nanoparticles (SLNs) comprise a versatile drug delivery system that has been developed for the treatment of a variety of diseases. The present study will investigate the feasibility of entrapping an active doxorubicin prodrug (a squalenoyl-derivative) in SLNs. The doxorubicin derivative-loaded SLNs are spherically shaped, have a mean diameter of 300–400 nm and show 85% w/w drug entrapment efficiency. The effects on cell growth of loaded SLNs, free doxorubicin and the prodrug have been examined using cytotoxicity and colony-forming assays in both human ovarian cancer line A2780 wild-type and doxorubicin-resistant cells. Further assessments as to the treatment’s ability to induce cell death by apoptosis have been carried out by analyzing annexin-V staining and the activation of caspase-3. The in vitro data demonstrate that the delivery of the squalenoyl-doxorubicin derivative by SLNs increases its cytotoxic activity, as well as its apoptosis effect. This effect was particularly evident in doxorubicin-resistant cells.

Development and Characterization of Solid Lipid Nanoparticles Loaded with a Highly Active Doxorubicin Derivative

Stella, Barbara
Co-first
;
Peira, Elena
Co-first
;
Dianzani, Chiara;Gallarate, Marina;Battaglia, Luigi;Dosio, Franco
2018

Abstract

Solid lipid nanoparticles (SLNs) comprise a versatile drug delivery system that has been developed for the treatment of a variety of diseases. The present study will investigate the feasibility of entrapping an active doxorubicin prodrug (a squalenoyl-derivative) in SLNs. The doxorubicin derivative-loaded SLNs are spherically shaped, have a mean diameter of 300–400 nm and show 85% w/w drug entrapment efficiency. The effects on cell growth of loaded SLNs, free doxorubicin and the prodrug have been examined using cytotoxicity and colony-forming assays in both human ovarian cancer line A2780 wild-type and doxorubicin-resistant cells. Further assessments as to the treatment’s ability to induce cell death by apoptosis have been carried out by analyzing annexin-V staining and the activation of caspase-3. The in vitro data demonstrate that the delivery of the squalenoyl-doxorubicin derivative by SLNs increases its cytotoxic activity, as well as its apoptosis effect. This effect was particularly evident in doxorubicin-resistant cells.
8
2
110
125
http://www.mdpi.com/2079-4991/8/2/110
anticancer agent, doxorubicin, solid lipid nanoparticles, cancer cells, nanoassemblies, anticancer prodrugs
Stella, Barbara; Peira, Elena; Dianzani, Chiara; Gallarate, Marina; Battaglia, Luigi; Gigliotti, Casimiro Luca; Boggio, Elena; Dianzani, Umberto; Dosio, Franco
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1660390
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