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

• Published in: Journal of nanoparticle research : an interdisciplinary forum for nanoscale science and technology Vol. 23; no. 7
• Main Authors: Halevas, Eleftherios, Mavroidi, Barbara, Kokotidou, Chrysoula, Mitraki, Anna, Pelecanou, Maria, Sagnou, Marina
• Format: Journal Article
• Language: English
• Published: Dordrecht Springer Netherlands 01-07-2021; Springer Nature B.V
• Subjects: Anticancer properties; Antitumor activity; Artemisinin; Bioavailability; Biocompatibility; Breast cancer; Cage molecules; Cancer; Characterization and Evaluation of Materials; Chemistry and Materials Science; Copolymers; Dendritic structure; Encapsulation; Entrapment; Fibroblasts; Hydrophobicity; Inorganic Chemistry; Lasers; Liquid phases; Materials Science; Nanomaterials; Nanotechnology; Natural products; Optical Devices; Optics; Pharmacophores; Photonics; Physical Chemistry; Polyethylene glycol; Propionic acid; Research Paper; Scaffolds; Tumor cell lines; Drug encapsulation; Drug delivery; Dendritic–linear–dendritic hybrid copolymers; Artemisinin; Anticancer activity; 2,2-Bis(hydroxymethyl)propionic acid hyperbranched dendritic nanocarriers
• ISSN: 1388-0764; 1572-896X
• DOI: 10.1007/s11051-021-05250-0

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.
Graphical abstract