Novel therapeutic modalities and drug delivery - erlotinib liposomes modified with galactosylated lipid: in vitro and in vivo investigations

The aim of this study to develop galactosylated erlotinib liposomes for treatment of lung cancer. The liposomes were prepared by using solvent evaporation method. Various parameters such as particle size, zeta potential, entrapment efficiency, stability and in vitro drug release were determined. The size of liposomes (both conventional and modified) was 103.5 and 121.4 nm. The zeta potential and EE of both liposomes were -7.1 +/- 1.3 mV, -1.2 +/- 0.5 mV and (82.3 +/- 1.9)%, (83.4 +/- 1.5)%, respectively. It was found that modified liposomes increase the size of particles. The in vitro release results indicated that the release of erlotinib from galactosylated liposomes was similar to that of conventional liposome, demonstrating that the modification did not affect erlotinib release. From the result of in vivo, it proved that erlotinib liposomes can significantly improve the drug targeting, rapidly distribute the drug in the body, prolong the drug circulation time and significantly increase the relative bioavailability of the drug. Biodistribution studies showed that erlotinib from galactosylated liposomes had higher AUC inside liver than the injection group and no histological change occurred to the rat liver after the administration of erlotinib conventional and galactosylated liposomes.