Published January 1, 2019
| Version v1
Journal article
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Inclusion of Quercetin in Gold Nanoparticles Decorated with Supramolecular Hosts Amplifies Its Tumor Targeting Properties
Creators
- 1. Selcuk Univ, Dept Chem, TR-42075 Konya, Turkey
- 2. Univ Ioannina, Dept Mat Sci Engn, Univ Campus, GR-45110 Ioannina, Greece
- 3. Univ Ioannina, Dept Chem, Lab Organ Chem & Biochem, GR-45110 Ioannina, Greece
- 4. Univ Ioannina, Fdn Res & Technol Hellas, Inst Mol Biol & Biotechnol, Dept Biomed Res, GR-45110 Ioannina, Greece
- 5. Univ Piemonte Orientale, Dipartimento Sci Salute, I-28100 Novara, Italy
- 6. Natl & Kapodistrian Univ Athens, Dept Chem, Athens 15571, Greece
- 7. Selcuk Univ, Dept Biochem, TR-42075 Konya, Turkey
Description
Despite the anticancer potential of natural products (NPs), their limited bioavailability necessitates laborious derivatization or covalent conjugation to delivery vehicles. To unleash their potential, we developed a nanohybrid delivery platform with a noncovalently tunable surface. Initially, the active compound was encapsulated in a macrocycle, p-sulfonatocalix[4]arene, enabling a 62 000-fold aqueous solubility amplification as also a 2.9-fold enhancement in its cytotoxicity with respect to the parent compound in SW-620 colon cancer cells. A pH stimuli responsive behavior was recorded for this formulate, where a programmable release of quercetin from the macrocycle was monitored in an acidic environment. Then, a nanoparticle gold core was decorated with calixarene hosts to accommodate noncovalently NPs. The loaded nanocarrier with the NP quercetin dramatically enhanced the cytotoxicity (>50-fold) of the parent NP in colon cancer and altered its cell membrane transport mode. In vivo experiments in a mouse 4T1 tumor model showed a reduction of tumor volume in mice treated with quercetin-loaded nanoparticles without apparent toxic effects. Further analysis of the tumor-derived RNA highlighted that treatment with quercetin-loaded nanoparticles altered the expression of 27 genes related to apoptosis.
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