Planta Med 2013; 79 - PN12
DOI: 10.1055/s-0033-1352356

Liposomes for dihydroartemisinin delivery to cancer cells: development, characterization and in vitro studies

C Righeschi 1, M Coronnello 2, A Mastrantoni 1, M Bergonzi 1, A Bilia 1
  • 11University of Florence, Department of Chemistry, via Ugo Schiff 6, 50019, Sesto Fiorentino, Florence, Italy
  • 22University of Florence, Department of Neuroscience, Pharmacology and Child's Health (NEUROFARBA), Viale Pieraccini 6, 50139, Florence, Italy

Dihydroartemisinin (DHA) is the most potent anticancer artemisinin-like compound and induce cancer cell death by apoptotic pathways; it is a poorly water soluble compound with low bioavailability and low half-life (34 – 90 min). Therefore, the development of the new formulation of DHA that enables quick availability to the body is of great need.

Conventional and stealth liposomes prepared according to the film hydration method, were fully characterized by particle size, zeta potential, polydispersity index, drug entrapment efficiency and TEM analysis. Stability in presence of blood proteins like albumin was evaluated. Cellular uptake of liposomes by flow cytometry and fluorescence microscopy analysis was investigated. In addition in vitro cytotoxicity studies in the cell line MCF-7 were carried out by sulforhodamine B assay.

Both formulations showed average size around 100nm and good values of zeta potential (-30 mv) and encapsulation efficiency (70%). TEM analysis confirmed the presence of round-shape vesicles that remain stable and intact also in presence of albumin. The higher cytotoxicity of conventional liposomes (IC50= 48.2µM) compared with stealth liposomes (IC50= 77µM) was consistent with the notion that pegylated liposomes might not interact directly with the tumor cells.

The two liposome formulations developed represent a successful attempt to incorporate dihydroartemisinin in liposomes with physical characteristics as drug carrier for parental administration.