Preparation and evaluation of folate-modified albumin baicalin-loaded nanoparticles for the targeted treatment of breast cancer

Abstract Baicalin (BA) has been shown to be one of the natural compounds with anti-proliferative activity against numerous cancer cell lines, but its application is restricted due to its rapid metabolism and non-targeting to specific tissues. This study exploited folic acid (FA)-conjugated bovine serum albumin (BSA) nanoparticles (NPs) loaded with baicalin (FA-BSANPs/BA) by desolvation crosslinking method to improve its bioavailability and therapeutic efficacy. The optimized FA-BSANPs/BA showed spherical shape and uniform distribution. The average particle size, zeta potential, encapsulation efficiency (EE) and drug loading (DL) of FA-BSANPs/BA were 228.41 ± 2.36 nm, −32.70 ± 1.27 mV, 76.88 ± 0.59% and 7.41 ± 0.23%, respectively. X-ray diffraction (XRD) and thermogravimetric (TG) analysis exhibited that the drug was amorphous in the particles. The results of drug release behavior in vitro demonstrated that FA-BSANPs/BA releases BA slowly and continuously. In vitro cytotoxicity test results suggested that the IC50 of FA-BSANPs/BA and BA on MCF-7 cells was 16.7 and 75.96 μg/mL, respectively. The uptake efficiency of FA-BSANPs was significantly higher than that of BSANPs, which leads to a stronger potential for apoptosis. In vivo antitumor studies showed that FA-BSANPs/BA can greatly inhibit tumor growth compared with BA and exhibited the ability to target tumors in MCF-7 xenograft tumor-bearing nude mice. In conclusion, FA-BSANPs/BA improves therapeutic efficacy of BA and reduces side effects by targeting tumors, providing a promising strategy for breast cancer therapy.