Development of Folate-Superparamagnetic Nanoconjugates for Inhibition of Cancer Cell Proliferation

Here, a versatile strategy to engineer smart theranostic nanocarriers is reported. The core/shell nanosystem is composed of a superparamagnetic iron oxide (Fe3-delta O4) nanoparticle (NP) core bearing the biocompatible thermo-responsive poly(2-(2-methoxy)ethyl methacrylate-oligo(ethylene glycol methacrylate), P(MEO(2)MA(x)-OEGMA(100-)(x)) copolymer (where x and 100-x represent the molar fractions of MEO(2)MA and OEGMA, respectively). Folic acid (FA) is end-conjugated to the P(MEO(2)MA(x)-OEGMA(100-)(x)) copolymer, leading to Fe-3-O-delta(4)@P(MEO(2)MA(x)-OEGMA(100-)(x))-FA, to facilitate active targeting of NPs to cancer cells. A highly potent hydrophobic anticancer agent doxorubicin (DOX) is incorporated in the thermo-responsive P(MEO(2)MA(x)-OEGMA(y)) brushes via supramolecular interactions to increase its solubility and the assessment of therapeutic potentials. These experiments confirm the magnetic hyperthermia properties of nanocarrier and reveal that only a small amount (10% +/- 4%) of DOX is diffused at room temperature, while almost full drug (100%) is released after 52 h at 41 degrees C. Interestingly, it is found that P(MEO(2)MA(60)-OEGMA(40)) polymers offer to NPs a promising stealth behavior against Human Serum Albumin and Fibrinogen model proteins.

Automated summary

A versatile strategy for engineering smart theranostic nanocarriers is reported in this study. The nanosystem consists of a superparamagnetic iron oxide (Fe3-delta O4) nanoparticle core and a biocompatible thermo-responsive copolymer shell. Folic acid is end-conjugated to the copolymer to enable active targeting of the nanocarriers to cancer cells. The incorporation of the hydrophobic anticancer drug doxorubicin in the thermo-responsive polymer brushes increases its solubility and therapeutic potential.