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. (c) 2012 Elsevier B.V. All rights reserved.