In this study, we report an active targeting liposomal formulation directed by a novel
peptide (RGD) that specifically binds to the
integrins receptors overexpressed on
prostatic cancer cells. The objectives of this study were to evaluate the in vitro and in vivo
tumor drug targeting delivery of RGD modified
liposomes on PC-3 cells and DU145 cells. The uptake efficiency of RGD-LP was 5.2 times higher than that of LP on PC-3 cells. The uptake efficiency of RGD-LP was 3.2 times higher than that of LP on DU145 cells. The anti-proliferative activity of RGD-LP-PTX against PC-3 cells and DU145 cells were much stronger compared to that of LP-PTX and free PTX, respectively. The
tumor spheroids experiment revealed that RGD-LP-PTX was more efficaciously internalized into
tumor spheroids than LP in both PC-3 cells and DU145 cells. Compared to LP-PTX and free PTX, RGD-LP-PTX showed the greatest
tumor growth inhibitory effect in vivo. In brief, the RGD-LP may be an efficient targeting drug delivery system for
prostatic cancer.