A facile preparation of novel multifunctional vectors by non-covalent bonds for co-delivery of doxorubicin and gene

In this study, novel multifunctional ternary complexes of biotinylated transferrin–avidin–biotin–poly(ethylene glycol)–poly(l-glutamate acid)/poly(2-(2-aminoethylamino) ethyl methacrylate)/doxorubicin–poly(l-aspartic acid)/pDNA (TAB/PIC–D/pDNA complexes) were prepared based on polyion complex micelles (PIC) and the avidin–biotin system, which aimed to target co-delivery of anti-cancer doxorubicin and gene. Cytotoxicity studies revealed that PIC–D could have anti-tumor effect on HeLa cells and HepG2 cells; TAB coating could increase the biocompatibility of PIC–D/pDNA complexes and the targeting delivery efficiency of doxorubicin. TAB/PIC–D/pDNA complexes possessed higher transfection efficiency than the unmodified complexes in serum, and transferrin could enhance luciferase expression in HeLa cells and HepG2 cells. Furthermore, confocal laser scanning microscopy showed that doxorubicin and gene could be delivered into HepG2 cells simultaneously by TAB/PIC–D/pDNA complexes. The formation of the ternary complexes provides a facile approach to constructing a multifunctional delivery system for targeted co-delivery of anticancer drugs and gene.