Formulation and Evaluation of Liposomes Containing Sorafenib Tosylate

The aim of the present study is to encapsulate Sorafenib tosylate in liposomal formulation for the effective treatment of hepatocellular carcinoma. Many conventional dosage forms of Sorafenib tosylate are available in market with high drug dose owing to high permeability and low solubility. But the large drug doses are coupled with a number of toxicities. To overcome such problems, the liposomal inclusions of Sorafenib tosylate have approached with the objective of increasing its bioavailability with small drug dose and better tumor targeting by making as a nano-sized formulation. The compatibility study of drug with phospholipids & other excipient have checked using the FTIR technique. In the present study, Sorafenib tosylate liposomes have prepared by thin film hydration technique using soyalecithin as lipid coat, cholesterol as rigidator, tween 80 and organic solvent like chloroform and methanol with hydrating media phosphate buffer (pH 7.4). Six formulations of liposomes have formulated, characterized and evaluated by particle size of vesicles, zeta potential, surface morphology, entrapment efficiency, invitro drug release and stability studies. The optimized formulation containing drug, lipid and cholesterol ratio 1:8:3 respectively, showed highest entrapment efficiency (55.62%). The optimized formulation has exhibited 83.36 % drug release within 24 hours. The stability study as per ICH guidelines at different temperatures conducted has showed maximum liposomal drug retention at refrigerated temperature 4ºC as compared to room temperature and accelerated stability study. The results suggest that the liposome encapsulation can increase the bioavailability of highly potent poorly bioavailable Sorafenib tosylate and can be used as a useful targeted drug delivery system for an effective management of hepatocellular carcinoma.