Transferrin (Tf) was immobilized onto Fe 3 O 4 @SiO 2 nanoparticles with high doxorubicin (DOX) loading (TfDMP), for dual targeting of cancer, by chemically coupling both Tf and DOX with dual-function magnetic nanoparticles (DMPs) using a multi-armed crosslinker, poly-L-glutamic acid. With high trapping efficiency for magnetic targeting, TfDMP exhibits a Tf receptor-targeting function. Moreover, the DOX loading percentage of TfDMP is high, and can be controlled by adjusting the reactant ratio. TfDMP presents a narrow size distribution, and is sensitive to pH for drug release. Compared with DOX-coupled DMP without Tf modification (DDMP), TfDMP exhibits enhanced uptake by Tf receptor-expressing tumor cells, and displays stronger cancer cell cytotoxicity. This study provides an efficient method for the dual-targeted delivery of therapeutic agents to tumors, with controlled low carrier toxicity and high efficiency.

Folate-modified iron ferrite nanoparticles with high doxorubicin loading (FDMP) were developed for dual targeting of tumor cells. Large quantities of doxorubicin and folate ligand were chemically coupled to the synthesized dual-functional magnetic nanoparticles by using the multihand cross-linker poly-L-glutamic acid. FDMP exhibits high drug loading ability, narrow size distribution and pH sensitivity to drug release. The drug loading ratio and the magnetic response can be adjusted by controlling the reactant ratio. FDMP possesses high magnetic-guided ability and exhibits enhanced uptake by folate receptors expressing tumor cells and increased cancer cell cytotoxicity.

A novel drug delivery system c(RGDyK)-modified Fe3O4 nanoparticles with high DOX load (R-DMP), which combines magnetic targeting, integrin alpha(v)beta3 targeting and high drug loading properties, was developed by chemical coupling both doxorubicin and peptide c(RGDyK) on the synthetic dual function magnetic nanoparticles (DMP) using a multi-hand cross-linker poly-L-glutamic acid. R-DMP has high drug loading ratio and trapping efficiency for magnetic targeting, and the drug loading ratio can be controlled by adjusting the reactant ratio. Moreover, R-DMP presents narrow size distribution and is sensitive to pH for drug releasing. Compare with those of doxorubicin coupled DMP without peptide c(RGDyK) modification, D-DMP shows enhanced uptake by integrin alpha(v)beta3 targeting expressing tumor cells and displays stronger cancer cell cytotoxicity. This investigate provides a new approach for the dual-targeted delivery of therapeutic agents to tumors with controlled low carrier toxicity and high efficiency.

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