Advanced bis-MPA hyperbranched dendritic nanocarriers of artemisinin with anticancer potential

In this work, a dendritic–linear–dendritic hybrid copolymer based on hyperbranched 2,2-bis(hydroxymethyl)propionic acid (bis-MPA) and linear polyethylene glycol (PEG) chain was employed for the encapsulation of artemisinin, a natural bioactive product with proven anticancer properties. The incorporation of artemisinin in the hyperbranched dendritic nano-scaffolds was accomplished via the “molecular encapsulation process” in the liquid phase. The nano-formulations obtained were evaluated for their structural and textural properties and were characterized by high entrapment efficiency and loading capacity and quantitative in vitro release of their load. They were completely soluble in physiological media and enhanced the solubility of hydrophobic artemisinin. The novel nanomaterials were further biologically evaluated for their degree of anticancer activity in two breast cancer cell lines, namely, MCF-7 and MDA-231, with healthy fibroblasts serving as control. The findings show that the novel nano-formulations maintain the anticancer activity of artemisinin, while they are completely non-toxic towards healthy fibroblasts, demonstrating for the first time the potential of the bis-MPA hyperbranched dendritic scaffolds as carriers and bioavailability enhancers of hydrophobic natural products and pharmacophores.