Tumor Targeting Gene Vector for Visual Tracking of Bcl-2 siRNA Transfection and Anti-Tumor Therapy.

Tumor targeting provided more effective gene therapy. Bcl-2 is an oncogene and Bcl-2 small interfering RNA (Bcl-2 siRNA) can inhibit its expression. Here a fluorescent and gene loading capacity vector DPL, derived from diketopyrrolopyrrole (DPP) was developed for Bcl-2 siRNA targeted delivery and tumor imaging in vitro and in vivo. The vector DPL showed a significant emission enhancement after interacting with siRNA, which was used to track the gene transfer process. Compared to commercial transfection reagent Lipo 2000, DPL obviously downregulated the Bcl-2 protein expression and exhibited excellent antitumor efficacy with less Bcl-2 siRNA. Importantly, DPL can target tumors to transport Bcl-2 siRNA to tumor sites in vivo based on enhanced permeability and retention (EPR) effect for effective in vivo tumor therapy. This work inspired us to design and synthesize multifunctional gene vector for tumor targeting and gene therapy.