The discovery that a
cane toad
poison-derived
steroid,
bufalin can significantly impact
cancer cell proliferation supports its potential use in
cancer therapy. However, its poor aqueous solubility and tissue deposition characteristics hamper its broader application as an anticancer therapeutic agent in its own right. To address this we developed an amphiphilic
dendrimer-based delivery system, which self-assembles into discrete
micelles in an aqueous environment. The
bufalin-
micelle inclusion complex was prepared by the co-precipitation method and their presence was confirmed by dynamic light scattering (DLS), zeta potential and differential scanning calorimetry (DSC) and transmission electron microscopy (TEM) measurements. The self-assembled
bufalin-containing
micelles were found to form at/above the
dendrimer concentration of 105.38 μmol L-1, and showed a more than threefold increase in the aqueous solubility (142.9 μg mL-1) of
bufalin, when compared with a saturated
bufalin aqueous
solution (42.4 μg mL-1), and two non-assembling
peptides of similar composition (79.3 and 62.5 μg mL-1 respectively).