Supercritical antisolvent process-assisted fabrication of chrysin-polyvinylpyrrolidone sub-microparticles for improved anticancer efficiency

The practical application of chrysin (CHS) is significantly hindered due to its poor aqueous solubility. To address this issue, a delivery platform based on CHS-polyvinylpyrrolidone (CHS-PVP) sub-microparticles was fabricated using the supercritical antisolvent (SAS) process. Initially, the effects of different operating parameters, including temperature, CHS concentration, and acetone/ethanol ratio on the particle size of CHS-PVP sub-microparticles were validated. This eco-friendly approach resulted in spherical-shaped particles with an average particle size of 273.7 nm +/- 38.9 nm at the optimal conditions: acetone/ethanol ratio of 3:7; CHS concentration of 3 mg/mL; and temperature of 318.15 K. Further, the molecular interactions, crystallinity, drug release, and anticancer efficiency in vitro of designed particles were systematically investigated. The CHS-PVP sub-microparticles exhibited higher antiproliferative effects over pure CHS in MDA-MB-231 cells, attributing to the enhanced solubility of CHS. These findings state that the SAS process-based CHS-PVP sub-microparticles have great potential in pharmaceutical applications. (C) 2020 Elsevier B.V. All rights reserved.