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.

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Methotrexate (MTX) is widely used for the treatment of various types of cancer; however, it has drawbacks such as low solubility, lack of selectivity, premature degradation, and side effects. To solve these weaknesses, a hydrogel with the ability to contain and release MTX under physiological conditions without burst release was synthesized. The hydrogel was fabricated with a poly(ɛ-caprolactone)-b-poly(ethylene glycol)-b-poly(ɛ-caprolactone) (PCL–PEG–PCL) triblock copolymer, synthesized by ring-opening polymerization. The characterizations by proton nuclear magnetic resonance spectroscopy and Fourier-transform infrared spectrometry confirmed the copolymer assembly, whereas the molecular weight analysis validated the PCL2000–PEG1000–PCL2000 structure. The copolymer aqueous solution exhibited sol–gel phase transition at 37°C and injection capacity. The hydrogel supported a load of 1,000 μg MTX·mL−1, showing a gradual and sustained release profile of the drug for 14 days, with a delivery up to 92% at pH 6.7. The cytotoxicity of the MTX-loaded hydrogel was performed by the methyl thiazole tetrazolium assay, showing a mean inhibitory concentration of 50% of MCF-7 cells (IC50) at 43 µg MTX·mL−1.