Saikosaponin-a loaded methoxy poly(ethylene glycol)-poly(ε-caprolactone) nanoparticles for improved solubility and reduced hemolysis of Saikosaponin-a

Methoxy poly(ethylene glycol)-poly(ε-caprolactone) (MePEG-PCL) nanoparticles (NPs) were fabricated using an emulsion solvent evaporation technique, aiming at improving the limited clinical application of Saikosaponin-a (SSa) due to its poor water solubility and hemolysis. The mean diameter of SSa loaded MePEG-PCL NPs (MePEG-PCL@SSa) were determined to be 97.02 ± 1.17 nm. The results of 1H NMR confirmed the core-shell structure of NPs. In vitro release of SSa from MePEG-PCL@SSa NPs was a sustained manner with no apparent initial drug burst. The hemolysis and cytotoxicity of MePEG-PCL@SSa were investigated with Red Blood Cells (RBC) and bEnd.3 cells, respectively. The results displayed that hemolysis reduced greatly (3.26 ± 0.17% at high NPs concentration), and the cytotoxicity was not seriously observed. Our findings provided a promising method to develop a SSa formulation for the potential clinical application.