Active targeting carrier for breast cancer treatment: Monoclonal antibody conjugated epirubicin loaded nanoparticle

Abstract Targeted nanomedicine plays an essential role in cancer therapy by delivering the drug to the malignant tumor cells directly. In this study, one of the potent anthracyclines, epirubicin (EPI), has been encapsulated in PLGA nanoparticles (NPs) conjugated by trastuzumab, as a monoclonal antibody (mAb). NPs was prepared by using nanoprecipitation technique. Characterizations have been performed by means of PCS, SEM, FT-IR and DSC techniques and then the optimum nanoparticles have been conjugated to mAb by an amide linkage. The results of the NPs preparation method showed the percentage yield of more than 90.55 ± 10.50% and entrapment efficiency of 91.05 ± 8.75%. PCS results showed that the average size of prepared NPs is approximately 74.66 ± 9.29 nm and 141 ± 58.41 nm for unconjugated and conjugated NPs respectively and a monodisperse distribution of them has been depicted by SEM micrograph. In vitro cellular experiments on overexpressing human epidermal growth factor receptor 2 (HER2) positive and negative cell lines demonstrated that mAb conjugated EPI-NPs has more cytotoxicity and drug uptake on over-expressed HER2 receptor cells in comparison to HER2 negative ones. The results of the current study have been demonstrated that targeted nanotechnology based formulations of EPI exhibit superior anticancer activity and have enormous potential in breast cancer (BC) treatment.