Glucose targeted therapy against liver hepatocellular carcinoma: In vivo study

Journal of Drug Delivery Science and Technology(2019)

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摘要
In this study, glucose-targeted and glucose-free micelles composed of a diblock copolymer of poly(ethylene glycol)-b-poly(lactide) that encapsulated superparamagnetic iron oxide (SPIO) and doxorubicin (DOX) in their hydrophobic core were fabricated. Glucose micelles showed 5.01 ± 0.3% drug loading content and 103 ± 4.0 nm size. We also endeavoured to observe the cellular uptake of these targeted and non-targeted micelles. The anticancer efficacy of the targeted, non-targeted micelles and free doxorubicin at the equivalent dose of 32 mg/kg were evaluated on the nude mice bearing tumours. Glucose micelles exhibited significant anticancer effects than free doxorubicin and non-targeted micelles. It was noteworthy that free doxorubicin showed toxicity at the site of injection. H&E staining of targeted micelles demonstrated remarkable changes in tumour architecture, also exerted higher percentage of necrosis (82.5%). Prussian blue staining revealed that tumour tissues with glucose DOX/SPIO micelles displayed much higher iron density than the non-targeted micelles, which could be employed for imaging tumour growth in the future. The data revealed that glucose targeted therapy can inhibit hepatocellular carcinoma when compared to non-targeted micelles. These specialised targeted micelles can serve as a theranostic agent hence, suggesting a useful targeted therapeutic and imaging strategy against liver cancer.
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关键词
Glucose DOX/SPIO micelles,Doxorubicin,Targeted micelles,HepG2,Anticancer activity
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