Synthesis of methotrexate-conjugated gold nanoparticles with enhanced cancer therapeutic effect

Tran, Ngoc; Wang, Tzu‐Hao; Lin, Chiao-Yun; Tai, Yian

doi:10.1016/j.bej.2013.04.017

Cited by 39 publications

(20 citation statements)

References 32 publications

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“…Moreover DL50 is twenty folds reduced at 72 h by the presence of nanoparticles conjugation. This result is in agreement with data reported by Chen et al for tumor cell lines [43] and for the first time we demonstrated the same behavior also on normal human keratinocytes.…”

Section: Growth Inhibitory Effect Of Methotrexate and Tests On Au-3mpsupporting

confidence: 94%

“…Only few papers report on the therapeutic effects of AuNPs as carriers of MTX and in particular in psoriasis treatment; one approach is based on the immobilization of the drug on AuNPs surface by means of a direct synthesis approach: the MTX can be used as a ligand and reducing agent for a one pot procedure, demonstrating an enhanced therapeutic effect of conjugated MTX, with cytotoxic effects in choriocarcinoma cell lines [43]. Alternatively, processes based on post-synthesis immobilization can be used and the conjugate shows an higher efficiency compared with an equal dose of free MTX with cytotoxic effects; in particular it inhibits tumor growth in a mouse ascites model of Lewis lung carcinoma [44].…”

Section: Introductionmentioning

confidence: 99%

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Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Bessar

Venditti

Benassi

et al. 2016

Colloids and Surfaces B: Biointerfaces

115

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a b s t r a c tGold nanoparticles (AuNPs) represent an effective choice for topical drug delivery systems thanks to their small size, general non-toxicity, ease of functionalization and high surface to volume ratio. Even if systemic, methotrexate still plays an important role in psoriasis treatment: its topical use shows insufficient percutaneus penetration owing to limited passive diffusion, high molecular weight and dissociation at physiological pH. The aim of our study was to design a new drug delivery nanocarrier for Methotrexate and to improve its solubility, stability and biodistribution. AuNPs were on purpose prepared with a hydrophilic stabilizing layer, in order to improve the colloidal stability in water. Watersoluble gold nanoparticles functionalized by sodium 3-mercapto-1-propansulfonate (Au-3MPS) were prepared and loaded with methotrexate (MTX). The loading efficiency of MTX on Au-3MPS was assessed in the range 70-80%, with a fast release (80% in one hour). The release was studied up to 24 h reaching the value of 95%. The Au-3MPS@MTX conjugate was fully characterized by spectroscopic techniques (UV-vis, FTIR) and DLS. Preliminary toxicity tests in the presence of keratinocytes monolayers allowed to assess that the used Au-3MPS are not toxic. The conjugate was then topically used on C57BL/6 mouse normal skin in order to trace the absorption behavior. STEM images clearly revealed the distribution of gold nanoparticles inside the cells. In vitro studies showed that Methotrexate conjugated with Au-3MPS is much more efficient than Methotrexate alone. Moreover, DL50, based on MTT analysis, is 20 folds reduced at 48 h, by the presence of nanoparticles conjugation. UV-vis spectra for in vivo tracing of the conjugate on bare mouse skin after 24 h of application, show increased delivery of Methotrexate in the epidermis and dermis using Au-3MPS@MTX conjugate, compared to MTX alone. Moreover we observed absence of the Au-3MPS in the dermis and in the epidermis, suggesting that these layers of the skin do not retain the nanoparticles. Based on our data, we found that the novel Au-3MPS@MTX conjugate is an effective non-toxic carrier for the satisfactory percutaneous absorption of Methotrexate and could help in possible topical treatment of psoriasis.

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Section: Growth Inhibitory Effect Of Methotrexate and Tests On Au-3mpsupporting

confidence: 94%

Section: Introductionmentioning

confidence: 99%

Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Bessar

Venditti

Benassi

et al. 2016

Colloids and Surfaces B: Biointerfaces

115

View full text Add to dashboard Cite

show abstract

“…Cell viability is observed to be ≈ 80% upon treatment with 2.0 ng/ml of Au NPs after a period of 48 h of incubation. Earlier reports have also shown that Au NPs have very little toxicity towards normal cells and are therefore preferred for various biological applications [52,53].…”

Section: = Cos … … (3)mentioning

confidence: 97%

Facile bio-synthesis of gold nanoparticles by using extract of Hibiscus sabdariffa and evaluation of its cytotoxicity against U87 glioblastoma cells under hyperglycemic condition

Mishra

Ray

Sinha

et al. 2016

Biochemical Engineering Journal

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“…It is an efficacious drug against psoriasis, rheumatism, melanoma and other types of cancer. 1 MTX is usually administered via oral or parenteral routes. 2 However, various side effects (stomatitis, 3 mucosal ulceration, bone-marrow suppression, 4 hepatic fibrosis/cirrhosis) 5 can occur if a commercial MTX formulation is administered over a long period.…”

Section: Introductionmentioning

confidence: 99%

<p>Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material</p>

Zhao¹,

Zheng²,

Wang³

et al. 2020

IJN

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Background: Methotrexate (MTX) is an antiproliferative drug widely used to treat inflammatory diseases and autoimmune diseases. The application of percutaneous administration is hindered due to its poor transdermal penetration. To reduce side effects and enhanced percutaneous delivery of MTX, novel methotrexate (MTX)-loaded micelles prepared with a amphiphilic cationic material, N,N-dimethyl-(N′,N′-di-stearoyl-1-ethyl)1,3-diaminopropane (DMSAP), was designed. Materials and Methods: DMSAP was synthesized via three steps using simple chemical agents. H nuclear magnetic resonance and mass spectroscopy were used to confirm the successful synthesis of DMSAP. A safe and non-toxic phosphatidylcholine, soybean phosphatidylcholine (SPC), was added to DMSAP at different ratios to form P/D-micelles. Then, MTX-entrapped micelles (M/P/D-micelles) were prepared by electrostatic adsorption. The physicochemical properties and blood stability of micelles were examined thoroughly. In addition, the transdermal potential of the micelles was evaluated by permeation experiments. Results: In aqueous environments, DMSAP conjugates could self-assemble spontaneously into micelles with a low critical micelle concentration (CMC) of 0.056 mg/mL. Stable, spherical MTX-entrapped micelles (M/P/D-micelles) with a size of 100-120 nm and high zeta potential of +36.26 mV were prepared. In vitro permeation studies showed that M/P/ D-micelles exhibited superior skin permeability and deposition of MTX in the epidermis and dermis compared with that of free MTX. Conclusion: These special novel cationic M/P/D-micelles can enhance the permeability of MTX and are expected to be a promising percutaneous delivery system for therapy skin diseases.

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Synthesis of methotrexate-conjugated gold nanoparticles with enhanced cancer therapeutic effect

Cited by 39 publications

References 32 publications

Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Functionalized gold nanoparticles for topical delivery of methotrexate for the possible treatment of psoriasis

Facile bio-synthesis of gold nanoparticles by using extract of Hibiscus sabdariffa and evaluation of its cytotoxicity against U87 glioblastoma cells under hyperglycemic condition

<p>Enhanced Percutaneous Delivery of Methotrexate Using Micelles Prepared with Novel Cationic Amphipathic Material</p>

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