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标题:Inclusion of Quercetin in Gold Nanoparticles Decorated with Supramolecular Hosts Amplifies its Tumor Targeting Properties
时间:2020-02-15 00:05:22
DOI:10.1021/acsabm.8b00748
作者:Yilmaz, Mustafa;Karanastasis, Apostolos A;Chatziathanasiadou, Maria V
关键词:cancer;in vivo;quercetin;calixarene;antitumor agents;drug delivery;natural products;nanoparticles
出版源: ACS Applied Bio Materials
摘要: Despite the anticancerpotential of natural products (NPs), theirlimited bioavailability necessitates laborious derivatization or covalentconjugation to delivery vehicles. To unleash their potential, we developeda nanohybrid delivery platform with a noncovalently tunable surface.Initially, the active compound was encapsulated in a macrocycle, <italic>p</italic>-sulfonatocalix­[4]­arene, enabling a 62 000-foldaqueous solubility amplification as also a 2.9-fold enhancement inits cytotoxicity with respect to the parent compound in SW-620 coloncancer cells. A pH stimuli responsive behavior was recorded for thisformulate, where a programmable release of quercetin from the macrocyclewas monitored in an acidic environment. Then, a nanoparticle goldcore was decorated with calixarene hosts to accommodate noncovalentlyNPs. The loaded nanocarrier with the NP quercetin dramatically enhancedthe cytotoxicity (>50-fold) of the parent NP in colon cancer andalteredits cell membrane transport mode. <italic>In vivo</italic> experimentsin a mouse 4T1 tumor model showed a reduction of tumor volume in micetreated with quercetin-loaded nanoparticles without apparent toxiceffects. Further analysis of the tumor-derived RNA highlighted thattreatment with quercetin-loaded nanoparticles altered the expressionof 27 genes related to apoptosis.
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页数:12 PAGES
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