Sorafenib, a multikinase inhibitor, has been clinically approved as the sole biological agent able to significantly improve survival in patients with advanced hepatocellular carcinoma (HCC), which are not candidates for surgical or ablative therapy. Although its effectiveness has been proven, the therapeutic response and application for local treatment of sorafenib is limited by its severe toxic side effects and poor solubility in aqueous environment [1]. Innovative alternative approaches for drug delivery is provided by the achievement of suitable nano-formulations which can promote the accumulation of high concentrations of drug to the targeted cancer sites, with a concomitant reduced toxicity of normal tissue. In this contest, superparamagnetic iron oxide NPs (SPIONs) were reported to improve the delivery of pharmacological agents to specific locations in the body through the application of an external magnetic field [2]. Here, solid lipid nanoparticles (SLNs) loaded with sorafenib and SPIONs were prepared and extensively investigated by complementary techniques, thus finally demonstrating their effectiveness as drug delivery magnetic nanovectors with good stability in aqueous medium and high drug encapsulation efficiency. In addition, a great potential of the use of the magnetic nanocarriers loaded with sorafenib as efficient contrast agents in magnetic resonance imaging was proven by phantom test. The here proposed lipid based magnetic nanoformulations loaded with sorafenib could be useful for the future image guided and magnetic targeting of sorafenib to liver towards an efficacious treatment of HCC.

Sorafenib loaded SLN magnetically targeting hepatoma

Nicoletta Depalo;Fabio Vischio;Marinella Striccoli;Maria Lucia Curri;
2018

Abstract

Sorafenib, a multikinase inhibitor, has been clinically approved as the sole biological agent able to significantly improve survival in patients with advanced hepatocellular carcinoma (HCC), which are not candidates for surgical or ablative therapy. Although its effectiveness has been proven, the therapeutic response and application for local treatment of sorafenib is limited by its severe toxic side effects and poor solubility in aqueous environment [1]. Innovative alternative approaches for drug delivery is provided by the achievement of suitable nano-formulations which can promote the accumulation of high concentrations of drug to the targeted cancer sites, with a concomitant reduced toxicity of normal tissue. In this contest, superparamagnetic iron oxide NPs (SPIONs) were reported to improve the delivery of pharmacological agents to specific locations in the body through the application of an external magnetic field [2]. Here, solid lipid nanoparticles (SLNs) loaded with sorafenib and SPIONs were prepared and extensively investigated by complementary techniques, thus finally demonstrating their effectiveness as drug delivery magnetic nanovectors with good stability in aqueous medium and high drug encapsulation efficiency. In addition, a great potential of the use of the magnetic nanocarriers loaded with sorafenib as efficient contrast agents in magnetic resonance imaging was proven by phantom test. The here proposed lipid based magnetic nanoformulations loaded with sorafenib could be useful for the future image guided and magnetic targeting of sorafenib to liver towards an efficacious treatment of HCC.
2018
Istituto per i Processi Chimico-Fisici - IPCF
hepatoma
drug delivery
nanoparticles
sorafenib
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/351232
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