Highly efficient delivery of therapeutic agents to target sites is of great importance for achieving ex
cellent therapeutic efficacy in cancer treatment. Here, we report a redox-responsive star-shaped magnetic mi
celle with both active-targeted and magnetic-guided functions. The magnetic star-shaped mi
celles are formed by self-assembly of four-arm poly(ethylene glycol) (PEG)-poly(ε-caprolactone) (PCL) copolymers with disulfide bonds as intermediate linkers. Anticancer drug doxorubicin (DOX) and magnetic iron oxide nanoparticles (Fe
3O
4) are simultaneously encapsulated into the hydrophobic cores. PBA ligands are chemically conjugated to the end of the hydrophilic PEG segments, endowing the active targeting of nanocarriers. Both qualitative and quantitative analyses of the intra
cellular uptake of these mi
celles with active-targeting and dual-targeting are performed
in vitro by cultured with salic acid (SA)-positive tumor
cells (human liver carcinoma
cell line HepG2, human cervical cancer
cell line HeLa) and SA-negative tumor
cells (human breast adenocarcinoma
cell line MCF-7, human non-small
cell lung cancer
cell line A549) in the presence or absence of a
permanent magnetic field.
In vivo biodistribution studies with active-targeting and dual-targeting and
in vivo anti-tumor effect are carried out in detail after being applied to the BALB/c mice bearing mouse H22 hepatocarcinoma
cells tumor model. These
in vivo results demonstrate that a great amount of dual-targeted magnetic mi
celles accumulate around the tumor tissues by the magnetic-guiding and in turn are taken up by the tumor
cells through SA-mediated endocytosis, leading to a high therapeutic efficacy to the artificial solid tumor.
Statement of Significance
A redox-responsive star-shaped magnetic micelle with both active-targeted and magnetic-guided functions was developed. Both qualitative and quantitative analysis of the intracellular uptake with dual-targeting of these micelles were performed in vitro by salic acid (SA)-positive tumor cells. The in vivo results demonstrate that a great amount of dual-targeted magnetic micelles accumulated around the tumor tissues, leading to a high therapeutic efficacy to artificial solid tumor.