Nanocomplexes from RGD-modified generation 1.0 polyamidoamine based copolymers used for intravascular gene release to prevent restenosis

Aim: To validate the efficacy of nanocomplexes from RGD-modified polyamidoamine (PAMAM G1) copolymer for prevention of restenosis. Materials & methods: Generation 1.0 polyamidoamine (PAMAM G1)-based copolymers (PGP) and RGD modified PGP (PGP-RGD) were synthesized and its properties were evaluated. Intravascular VEGF165 release tests were performed. Results: The PGP-RGD1 (2.6% grafting rate) exhibited lower cytotoxicity and larger combining ability with pDNA. The complexes had sizes of 80-160 nm and zeta potentials of 3-20 mV. Transfection efficiency of PGP-RGD1 complexes in human umbilical vein endothelial cells was larger than that of PGP complexes. Patency and expression level of artery in PGP-RGD1 group were higher than that in saline group. Conclusion: PGP-RGD1 will be a promising targeted gene vector.