Synthesis and in vitro biological evaluation as antitumour drug carriers of folate-targeted N-isopropylacrylamide-based nanohydrogels

Autor: Marta Benito, Elena Conde Pérez, Issa Katime, José M. Teijón, Rosa Olmo, César Teijón, María Dolores Blanco
Rok vydání: 2012
Předmět:
Zdroj: Polymer International. 61:1202-1212
ISSN: 0959-8103
DOI: 10.1002/pi.4200
Popis: Copolymeric nanohydrogels based on N-isopropylacrylamide, N-(pyridin-4-ylmethyl)acrylamide and tert-butyl-2acrylamidoethyl carbamate, synthesized by microemulsion polymerization, were characterized using Fourier transform infrared spectroscopy and their size (38 – 52 nm) determined using quasielastic light scattering. Folic acid was covalently attached to the nanohydrogels (1.40 ± 0.07 mmol g −1 ). Tamoxifen (6.7 ± 0. 2–7 .3 ± 1.2 µ gT MX mg −1 nanohydrogel), a hydrophobic anticancer drug, and 5-fluorouracil (7.7 ± 0. 7–1 0.14 ± 1.75 µ g5 -FU mg −1 nanohydrogel), a hydrophilic anticancer drug, were loaded into the nanohydrogels. Maximum invitro TMX release (77 – 84% of loaded drug) depended on interactions of the drug with hydrophobic clusters of the nanogels; however, no nanogel/5-FU interactions allowed total release of the loaded drug. The cytotoxicity of unloaded nanohydrogels in MCF7, T47D and HeLa cells was low. Cell uptake of nanogels without bound folic acid took place in the three cell types by unspecific internalization in a time-dependent process. Cell uptake increased for folic acid-targeted nanohydrogels in T47D and HeLa cells, which have folate receptors. The administration of 10 and 30 µmol L −1 TMX by TMX-loaded nanogels and 10 µmol L −1 5-FU by 5-FU-loaded nanogels was effective on the three cell types, and the best results were obtained for folic acid-targeted nanohydrogels. c � 2012 Society of Chemical Industry Supporting information may be found in the online version of this article.
Databáze: OpenAIRE
Externí odkaz: