Folic acid anchored urchin-like raloxifene nanoparticles for receptor targeting in breast cancer: Synthesis, optimisation and in vitro biological evaluation

Abstract

In this study, raloxifene hydrochloride (RLX) was loaded into bovine serum albumin nanoparticles (RLX-BSA-NPs) and further surface modified with folic acid (FA-RLX-BSA-NPs) for targeted breast cancer therapy. In statistical optimization of RLX-BSA-NPs, albumin and crosslinker concentration significantly affected particle size and entrapment efficiency of RLX-BSA-NPs. Structural characterizations confirmed that the formation of FA-RLX-BSA-NPs and SEM microphotographs resembled the urchin-like spiky feature. A sustained in vitro release pattern was observed till 120 h from FA-RLX-BSA-NPs in phosphate buffer. The MTT assay revealed maximum cell inhibition by FA-RLX-BSA-NPs against MCF-7 cells and MDA MB-231 cells at lower IC50 values (0.5 µg/ml and 0.7 µg/ml) compared to RLX and RLX-BSA-NPs. The cell cycle analysis revealed that FA-RLX-BSA-NPs induced apoptosis of MCF-7 cells in the sub-G1 phase via folate receptor-α mediated endocytic uptake. Hence, the raloxifene nanoparticles stance as a potential nanocarrier for targeted therapy in breast cancer.