A dual-targeting liposome conjugated with transferrin and RGD enhanced drug delivery across the blood-brain barrier and glioma targeting
Abstract
The treatment of a brain glioma is still one of the most difficult challenges in oncology. We developed in this research a delivery system for targeted drug delivery across the blood-brain barrier (BBB) and then targeted to the brain cancer cells. Herein, we utilize a cyclic RGD peptide and transferrin (TF) as targeting ligands. Cyclic RGD are specific targeting ligands of the cancer cells and transferrin are specific targeting ligands of both BBB and cancer cells. We conjugate them with liposome to establish the brain glioma cascade delivery system (RGD/TF-LP). The liposome were prepared by the film-ultrasonic method and characterized for their various physicochemical. In vitro cell uptake and three-dimensional tumor spheroid penetration studies demonstrated that the system could not only target endothelial and tumor cells but also penetrate the tumor cells to reach the core of the tumor spheroids. In vivo imaging further demonstrated that the RGD/TF-LP provided the highest brain distribution. As a result, the paclitaxel -loaded RGD/TF-LP presents the best anti-proliferative activity against C6s and tumor spheroids. In conclusion, the RGD/TF-LP could precisely target to the brain glioma, which was a valuable target for glioma imaging and therapy.
Key words: Dual targeting, cyclic RGD, transferrin, glioma

期刊是  德国   pharmazie  影响因子  1分

有意向客户请联系本站客服。