Folic acid-modified methotrexate-conjugated gold nanoparticles as nano-sized trojans for drug delivery to folate receptor-positive cancer cells

Methotrexate (MTX), an analog of folic acid (FA), is a drug widely used in cancer treatment. To prevent its potential toxicity and enhance therapeutic efficacy, targeted drug delivery systems, especially nanotechnology-folate platforms, are a central strategy. Gold nanoparticles (AuNPs) are promisin...

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Bibliographic Details
Published in:Nanotechnology 2020-08, Vol.31 (35), p.355101
Main Authors: Yücel, O uz, engelen, Asl han, Emik, Serkan, Önay-Uçar, Evren, Arda, Nazl, Gürda, Gülten
Format: Article
Language:English
Subjects:
A549 Cells
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
cancer therapy
Cell Line, Tumor
Cell Proliferation - drug effects
Cell Survival - drug effects
Drug Synergism
folate receptor
Folic Acid - chemistry
Folic Acid - pharmacology
Glutathione - chemistry
Gold - chemistry
gold nanoparticles
HEK293 Cells
HeLa Cells
Humans
Metal Nanoparticles
methotrexate
Methotrexate - chemistry
Methotrexate - pharmacology
Particle Size
PC-3 Cells
targeted drug delivery
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Summary:Methotrexate (MTX), an analog of folic acid (FA), is a drug widely used in cancer treatment. To prevent its potential toxicity and enhance therapeutic efficacy, targeted drug delivery systems, especially nanotechnology-folate platforms, are a central strategy. Gold nanoparticles (AuNPs) are promising candidates to be used as drug delivery systems because of their small particle sizes and their inertness for the body. In this study, glutathione (GSH)-coated FA-modified spherical AuNPs (5.6 nm) were successfully synthesized, and the anticancer activity of novel MTX-loaded (MTX/Au-GSH-FA) NPs (11 nm) was examined. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) results showed that MTX/AuNPs possess spherical morphology, nanoscaled particle size, narrow size distribution, and good stability. In vitro studies showed that cytotoxicity of MTX/Au-GSH-FA to folate receptor-positive (FR+) human brain (U-87 MG) and cervical (HeLa) cancer cells enhanced significantly (∼3 and ∼10 fold, respectively) compared to free MTX while there was no significant effect in FR−negative human cell lines A549 (lung carcinoma), PC3 (prostate carcinoma), HEK-293 (healthy embryonic kidney). Moreover, the receptor specificity of the conjugate was shown by fluorescent microscopic imaging. In conclusion, these results indicate that the synthesized novel MTX/Au-GSH-FA NP complex seems to be a good candidate for effective and targeted delivery in FR+ cancer therapy.
ISSN:0957-4484
1361-6528
DOI:10.1088/1361-6528/ab9395