3 years ago

Nucleoside-Lipid-Based Nanocarriers for Sorafenib Delivery

Philippe Barthélémy, Bruno Alies, Ananda Appavoo, Gaelle Vacher, Karen Gaudin, Ludivine Ferey, Sebastien Benizri, Cathy Staedel, Naila Mebarek

Abstract

Although the application of sorafenib, a small inhibitor of tyrosine protein kinases, to cancer treatments remains a worldwide option in chemotherapy, novel strategies are needed to address the low water solubility (< 5 μM), toxicity, and side effects issues of this drug. In this context, the use of nanocarriers is currently investigated in order to overcome these drawbacks. In this contribution, we report a new type of sorafenib-based nanoparticles stabilized by hybrid nucleoside-lipids. The solid lipid nanoparticles (SLNs) showed negative or positive zeta potential values depending on the nucleoside-lipid charge. Transmission electron microscopy of sorafenib-loaded SLNs revealed parallelepiped nanoparticles of about 200 nm. Biological studies achieved on four different cell lines, including liver and breast cancers, revealed enhanced anticancer activities of Sorafenib-based SLNs compared to the free drug. Importantly, contrast phase microscopy images recorded after incubation of cancer cells in the presence of SLNs at high concentration in sorafenib (> 80 μM) revealed a total cancer cell death in all cases. These results highlight the potential of nucleoside-lipid-based SLNs as drug delivery systems.

Publisher URL: https://link.springer.com/article/10.1186/s11671-017-2420-2

DOI: 10.1186/s11671-017-2420-2

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