pH-responsive polymer micelles for methotrexate delivery at tumor microenvironments
Fecha
2020-11-16Autor
Castro Carmona, Javier Servando
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Methotrexate (MTX) anticancer drug was successfully loaded and released in a controlled manner
from polymer micelles made of a diblock copolymer of
poly(monomethoxy ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL). The empty and MTX-loaded micelles
(MTX/mPEG-PCL) were characterized by electron microscopy. The drug release dependence upon pH 5.4, 6.5,
and 7.4 for 30 days was proven and characterized
by UV-Vis spectroscopy. The cytotoxic effect of MTX/
mPEG-PCL micelles on MCF-7 breast cancer cells was
evaluated through an MTT assay. The morphological analysis indicated the successful formation of micelles of 76
and 131 nm for empty and MTX-loaded micelles, respectively. An encapsulation efficiency of 70.2% and a loading
capacity of 8.8% were obtained. The in vitro release of MTX
showed a gradual and sustained profile over 22 days, with a
clear trend to much higher release at acidic pH (80 and
90% for pH 6.7 and 5.5, respectively). The MTX/mPEG-PCL
micelles showed an IC50 of MCF-7 cells at 30 µg mL−1
. The results suggested that MTX/mPEG-PCL could be a promising drug delivery system for cancer treatment