Folic acid and cell-penetrating peptide conjugated PLGA–PEG bifunctional nanoparticles for vincristine sulfate delivery

Dual- and multi-functional drug delivery systems , especially ligand-modified nanoparticles (NPs) loaded with chemotherapeutic agents are paid much attention to due to their excellent behavior in vitro and in vivo . Bifunctional NPs (BF-NPs), which were based on PLGA–PEG and modified with folic acid and cell penetrating peptide R 7 simultaneously, were developed. BF-NPs loaded with vincristine sulfate (VCR) were prepared via the water–oil–water emulsion solvent evaporation method. BF-NPs showed favorable particle size and zeta potentials , promising drug loading and entrapment efficiency. The release of VCR from BF-NPs exhibited a biphase release manner. Cellular uptake of BF-NPs was found to be higher than that of the NPs merely modified by folic acid or R 7 . In vitro cytotoxicity, cell apoptosis and cell cycle arrest studies also revealed that BF-NPs were more potent than those of the NPs merely modified by folic acid or R 7 . Therefore, the results demonstrated that BF-NPs developed in this study could be a potential vehicle for delivering chemotherapeutic agents such as VCR and breast cancer therapy.