TY - JOUR
T1 - Sorafenib delivery nanoplatform based on superparamagnetic iron oxide nanoparticles magnetically targets hepatocellular carcinoma
AU - Depalo, Nicoletta
AU - Iacobazzi, Rosa Maria
AU - Valente, Gianpiero
AU - Arduino, Ilaria
AU - Villa, Silvia
AU - Canepa, Fabio
AU - Laquintana, Valentino
AU - Fanizza, Elisabetta
AU - Striccoli, Marinella
AU - Cutrignelli, Annalisa
AU - Lopedota, Angela
AU - Porcelli, Letizia
AU - Azzariti, Amalia
AU - Franco, Massimo
AU - Curri, Maria Lucia
AU - Denora, Nunzio
PY - 2017/7/1
Y1 - 2017/7/1
N2 - Currently, sorafenib is the only systemic therapy capable of increasing overall survival of hepatocellular carcinoma patients. Unfortunately, its side effects, particularly its overall toxicity, limit the therapeutic response that can be achieved. Superparamagnetic iron oxide nanoparticles (SPIONs) are very attractive for drug delivery because they can be targeted to specific sites in the body through application of a magnetic field, thus improving intratumoral accumulation and reducing adverse effects. Here, nanoformulations based on polyethylene glycol modified phospholipid micelles, loaded with both SPIONs and sorafenib, were successfully prepared and thoroughly investigated by complementary techniques. This nanovector system provided effective drug delivery, had an average hydrodynamic diameter of about 125 nm, had good stability in aqueous medium, and allowed controlled drug loading. Magnetic analysis allowed accurate determination of the amount of SPIONs embedded in each micelle. An in vitro system was designed to test whether the SPION micelles can be efficiently held using a magnetic field under typical flow conditions found in the human liver. Human hepatocellular carcinoma (HepG2) cells were selected as an in vitro system to evaluate tumor cell targeting efficacy of the superparamagnetic micelles loaded with sorafenib. These experiments demonstrated that this delivery platform is able to enhance sorafenib’s antitumor effectiveness by magnetic targeting. The magnetic nanovectors described here represent promising candidates for targeting specific hepatic tumor sites, where selective release of sorafenib can improve its efficacy and safety profile. [Figure not available: see fulltext.].
AB - Currently, sorafenib is the only systemic therapy capable of increasing overall survival of hepatocellular carcinoma patients. Unfortunately, its side effects, particularly its overall toxicity, limit the therapeutic response that can be achieved. Superparamagnetic iron oxide nanoparticles (SPIONs) are very attractive for drug delivery because they can be targeted to specific sites in the body through application of a magnetic field, thus improving intratumoral accumulation and reducing adverse effects. Here, nanoformulations based on polyethylene glycol modified phospholipid micelles, loaded with both SPIONs and sorafenib, were successfully prepared and thoroughly investigated by complementary techniques. This nanovector system provided effective drug delivery, had an average hydrodynamic diameter of about 125 nm, had good stability in aqueous medium, and allowed controlled drug loading. Magnetic analysis allowed accurate determination of the amount of SPIONs embedded in each micelle. An in vitro system was designed to test whether the SPION micelles can be efficiently held using a magnetic field under typical flow conditions found in the human liver. Human hepatocellular carcinoma (HepG2) cells were selected as an in vitro system to evaluate tumor cell targeting efficacy of the superparamagnetic micelles loaded with sorafenib. These experiments demonstrated that this delivery platform is able to enhance sorafenib’s antitumor effectiveness by magnetic targeting. The magnetic nanovectors described here represent promising candidates for targeting specific hepatic tumor sites, where selective release of sorafenib can improve its efficacy and safety profile. [Figure not available: see fulltext.].
KW - drug delivery
KW - hepatocellular carcinoma
KW - magnetic targeting
KW - PEG-modified phospholipid micelles
KW - sorafenib
KW - superparamagnetic iron oxide nanoparticles
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U2 - 10.1007/s12274-017-1444-3
DO - 10.1007/s12274-017-1444-3
M3 - Article
AN - SCOPUS:85016124369
VL - 10
SP - 2431
EP - 2448
JO - Nano Research
JF - Nano Research
SN - 1998-0124
IS - 7
ER -