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 the enhanced permeability and retention (EPR) effect for effective in vivo tumor therapy. This work inspired us to design and synthesize a multifunctional gene vector for tumor targeting and gene therapy.