Niosomal nanocarriers for gemcitabine in treatment of MDA-MB-231, AsPC-1 and Calu-6 cells: investigations in vitro and in vivo

Gemcitabine (GEM) is a cytotoxic chemotheraputic agent employed for treatment of different cancers. GEM-loaded nanoniosomes were synthesized and characterized to enhance efficacy and weaken its side effects by decreasing half-maximal inhibitory concentration (IC50) value. The nanoniosomes were prepared through thin film hydration using cholesterol, and either Span 20 or Span 80, and GEM were loaded to prepare two nanoniosome formulations of GEM-Span 20 and GEM-Span 80, respectively. Size of particles, zeta potential, and efficiency of entrapment of GEM-Span 20 and GEM-Span 80 were measured to be 132 and 126 nm, 3.2 and −23 mV, and 71.4 and 73.1 %, respectively. Both nanoniosome formulations provided sustained GEM release in vitro under the Higuchi kinetic model. Cytotoxicity of the nanoniosome formulations was evaluated, and the results indicated 2.1, 4.7, and 9.4 time decrements in IC50 values of GEM-Span 80 toward MDA-MB-231, AsPC-1 and Calu-6 cells, respectively, compared to GEM solutions. Bioavailability of the nanoniosomes was also measured in vivo upon both intraperitoneal (IP) injection and oral administration, and the pharmacokinetic parameters were derived. Both in vitro and in vivo release studies indicated sustained GEM release from the nanoniosomes.