by Keyword: Antitumor drug
Maroni, Giorgia, Tomassi, Elena, Valenti, Donatella, Fernandez-Busquets, Xavier, Pucci, Laura, Levantini, Elena, Caddeo, Carla, (2024). Pegylated-liposomes increase the efficacy of Idelalisib in lymphoma B-cells International Journal Of Pharmaceutics 657, 124144 
New drugs and technologies are continuously developed to improve the efficacy and minimize the critical side effects of cancer treatments. The present investigation focuses on the development of a liposomal formulation for Idelalisib, a small-molecule kinase inhibitor approved for the treatment of lymphoid malignancies. Idelalisib is a potent and selective antitumor agent, but it is not indicated nor recommended for first-line treatment due to fatal and serious toxicities. Herein, liposomes are proposed as a delivery tool to improve the therapeutic profile of Idelalisib. Specifically, PEGylated liposomes were prepared, and their physicochemical and technological features were investigated. Light-scattering spectroscopy and cryo-transmission electron microscopy revealed nanosized unilamellar vesicles, which were proved to be stable in storage and in simulated biological fluids. The cytotoxicity of the liposome formulation was investigated in a human non-Hodgkin's lymphoma B cell line. Idelalisib was able to induce death of tumor cells if delivered by the nanocarrier system at increased efficacy. These findings suggest that combining Idelalisib and nanotechnologies may be a powerful strategy to increase the antitumor efficacy of the drug.
JTD Keywords: Antitumor drug, Apoptosis, Idelalisib, Liposomes, Lymphoma cells, Nanodeliver
