Background: Deguelin (DGL) is a natural flavonoid reported to exhibit
antitumor effects in breast cancer (BC). PEG-PCL (Polyethylene Glycol-
Polycaprolactone), as polymeric micelles, has biodegradability and
biocompatibility. The aim of this study was to investigate whether the
nanoparticular delivery system, PEG-PCL could improve the bioavailability of DGL
for suppressing proliferation of BC cells. Methods: PEG-PCL polymers
were first prepared by ring-opening polymerization, and DGL and paclitaxel (PTX)-loaded
PEG-PCL nano-micelles were formulated via the film dispersion method. The
composition and molecular weight of PEG-PCL were analyzed by nuclear magnetic
resonance and fourier Transform infrared spectroscopy (FTIR) spectra. Particle size, surface potential and hemolytic
activity of micelles were assessed by dynamic light scattering, transmission
electron microscopy and hemolysis assay, respectively. Then proliferation and
apoptosis of MDA-MB-231 and MDA-MB-468 cells were tested with Edu staining,
CCK-8, TUNEL staining, and Flow cytometer. Caspase 3 expression was also assessed
by Western blot. Results: Our results first indicated that
PEG