Next Article in Journal
Thermally Stimulated Currents in Nanocrystalline Titania
Next Article in Special Issue
Comparative Evaluation of U.S. Brand and Generic Intravenous Sodium Ferric Gluconate Complex in Sucrose Injection: Physicochemical Characterization
Previous Article in Journal
Organozinc Precursor-Derived Crystalline ZnO Nanoparticles: Synthesis, Characterization and Their Spectroscopic Properties
Previous Article in Special Issue
Covalent Organic Frameworks: From Materials Design to Biomedical Application
Article Menu
Issue 1 (January) cover image

Export Article

Open AccessArticle
Nanomaterials 2018, 8(1), 24; https://doi.org/10.3390/nano8010024

Enhanced and Selective Antiproliferative Activity of Methotrexate-Functionalized-Nanocapsules to Human Breast Cancer Cells (MCF-7)

1
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre 90610-000, RS, Brazil
2
Programa de Pós-Graduação em Química, Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre 91501-970, RS, Brazil
3
Programa de Pós-Graduação em Nanotecnologia Farmacêutica, Universidade Federal do Rio Grande do Sul, Porto Alegre 90610-000, RS, Brazil
*
Author to whom correspondence should be addressed.
Received: 3 November 2017 / Revised: 21 December 2017 / Accepted: 28 December 2017 / Published: 4 January 2018
(This article belongs to the Special Issue Pharmaceutical Nanotechnology)
Full-Text   |   PDF [1724 KB, uploaded 4 January 2018]   |  

Abstract

Methotrexate is a folic acid antagonist and its incorporation into nanoformulations is a promising strategy to increase the drug antiproliferative effect on human breast cancer cells by overexpressing folate receptors. To evaluate the efficiency and selectivity of nanoformulations containing methotrexate and its diethyl ester derivative, using two mechanisms of drug incorporation (encapsulation and surface functionalization) in the in vitro cellular uptake and antiproliferative activity in non-tumoral immortalized human keratinocytes (HaCaT) and in human breast carcinoma cells (MCF-7). Methotrexate and its diethyl ester derivative were incorporated into multiwall lipid-core nanocapsules with hydrodynamic diameters lower than 160 nm and higher drug incorporation efficiency. The nanoformulations were applied to semiconfluent HaCaT or MCF-7 cells. After 24 h, the nanocapsules were internalized into HaCaT and MCF-7 cells; however, no significant difference was observed between the nanoformulations in HaCaT (low expression of folate receptors), while they showed significantly higher cellular uptakes than the blank-nanoformulation in MCF-7, which was the highest uptakes observed for the drug functionalized-nanocapsules. No antiproliferative activity was observed in HaCaT culture, whereas drug-containing nanoformulations showed antiproliferative activity against MCF-7 cells. The effect was higher for drug-surface functionalized nanocapsules. In conclusion, methotrexate-functionalized-nanocapsules showed enhanced and selective antiproliferative activity to human breast cancer cells (MCF-7) being promising products for further in vivo pre-clinical evaluations. View Full-Text
Keywords: methotrexate; surface functionalized lipid-core nanocapsules; breast cancer; cellular uptake; antiproliferative activity methotrexate; surface functionalized lipid-core nanocapsules; breast cancer; cellular uptake; antiproliferative activity
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

De Oliveira, C.P.; Büttenbender, S.L.; Prado, W.A.; Beckenkamp, A.; Asbahr, A.C.; Buffon, A.; Guterres, S.S.; Pohlmann, A.R. Enhanced and Selective Antiproliferative Activity of Methotrexate-Functionalized-Nanocapsules to Human Breast Cancer Cells (MCF-7). Nanomaterials 2018, 8, 24.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Nanomaterials EISSN 2079-4991 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top