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Title: In vitro antitumor activity of methotrexate via pH-sensitive chitosan nanoparticles
Author: Nogueira, Daniele R.
Tavano, Lorena
Mitjans Arnal, Montserrat
Pérez Muñoz, Lourdes
Infante Martínez-Pardo, Ma. Rosa
Vinardell Martínez-Hidalgo, Ma. Pilar
Keywords: Agents tensioactius
Membranes cel·lulars
Citotoxicitat per mediació cel·lular
Surface active agents
Cell membranes
Cell-mediated cytotoxicity
Issue Date: Apr-2013
Publisher: Elsevier B.V.
Abstract: Nanoparticles with pH-sensitive behavior may enhance the success of chemotherapy in many cancers by efficient intracellular drug delivery. Here, we investigated the effect of a bioactive surfactant with pH-sensitive properties on the antitumor activity and intracellular behavior of methotrexate-loaded chitosan nanoparticles (MTX-CS-NPs). NPs were prepared using a modified ionotropic complexation process, in which was included the surfactant derived from Nα,Nε-dioctanoyl lysine with an inorganic lithium counterion. The pH-sensitive behavior of NPs allowed accelerated release of MTX in an acidic medium, as well as membrane-lytic pH-dependent activity, which facilitated the cytosolic delivery of endocytosed materials. Moreover, our results clearly proved that MTX-CSNPs were more active against the tumor HeLa and MCF-7 cell lines than the free drug. The feasibilty of using NPs to target acidic tumor extracellular pH was also shown, as cytotoxicity against cancer cells was greater in a mildly acidic environment. Finally, the combined physicochemical and pH-sensitive properties of NPs generally allowed the entrapped drug to induce greater cell cycle arrest and apoptotic effects. Therefore, our overall results suggest that pH-sensitive MTX-CS-NPs could be potentially useful as a carrier system for tumor and intracellular drug delivery in cancer therapy.
Note: Versió postprint del document publicat a:
It is part of: Biomaterials, 2013, vol. 34, núm. 11, p. 2758-2772
Related resource:
ISSN: 0142-9612
Appears in Collections:Articles publicats en revistes (Bioquímica i Fisiologia)

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