Abstract
Aim: Monascin and ankaflavin, the major fractions of the fungal-derived monascus yellow pigments, were incorporated with the herbal drug, resveratrol (RSV) within the core of folate-conjugated casein micelles (FA-CAS MCs, F1) for active targeting. PEGylated RSV-phospholipid complex bilayer enveloping casein-loaded micelles (PEGPC-CAS MCs) were also developed as passive-targeted nanosystem. Results: FA-and PEGPC-CAS MCs demonstrated a proper size with monomodal distribution, sustained drug release profiles and good hemocompatibility. The coloaded MCs showed superior cytotoxicity to MCF-7 breast cancer cells compared with free drugs. Both nanosystems exerted excellent in vivo antitumor efficacy in breast cancer bearing mice with PEGylated MCs showing comparable tumor regression to folate-conjugated MCs. Conclusion: Evergreen nanoplatforms coloaded with monascus yellow pigments and RSV were effective for breast cancer treatment.