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.