Effectiveness of Free and Liposome-Entrapped Antitumoral Drugs against Hepatocellular Carcinoma: A Comparative In vitro Study

Abstract

Hepatocellular carcinoma (HCC) is a highly prevalent form of liver cancer. Sorafenib is the first-line treatment for patients who are not eligible for surgical procedures. Still, it causes important adverse effects, does not provide symptoms relief, and is marketed at expensive costs. Here we investigated the effectiveness of imatinib, sunitinib, and bortezomib against an in vitro model of HCC. These drugs are less expensive than Sorafenib and are approved for other malignant neoplasia. The drugs were tested as free and liposome-entrapped forms against HepG2 cells. Liposomes were prepared without using organic solvents and were tested for physicochemical stability. Entrapment efficiency was determined by spectrophotometric methods. Liposomes' average size was 238±33 nm, with an average entrapment efficiency of 34.3%. All drugs significantly decreased the viability of HepG2 cells in their free form and liposome-entrapped forms compared to the control. In spite of the low entrapment efficiency, no organic solvent was used in liposomes preparation, and cell viability values after 18h treatments with liposome-entrapped drugs were only surpassed by the highest concentration of free drugs. Our data open doors for more studies to assess the safety of the liposomes in vivo.