Liposome formulation for delivery of Wnt signal pathway inhibitor

A liposome formulation for delivery of a Wnt signal pathway inhibitor, comprising lipid molecules encapsulating the Wnt signal pathway inhibitor,

• wherein:
• the Wnt signal pathway inhibitor encapsulated within the liposome formulation has a concentration between 0.6 mg/ml and 1.3 mg/ml;
• the Wnt signal pathway inhibitor is compound 28, having the structure
• or a pharmaceutically acceptable salt thereof;
• the lipid molecules are hydrogenated soybean lecithin, cholesterol, and distearoyl phosphatidylethanolamine-polyethylene glycol, and the molar ratio among hydrogenated soybean lecithin, cholesterol, and distearoyl phosphatidylethanolamine-polyethylene glycol is 55:5:40, and the molar ratio between the Wnt signal pathway inhibitor and the sum amount of hydrogenated soybean lecithin, cholesterol, and distearoyl phosphatidylethanolamine-polyethylene glycol is 1:10;
• and
• wherein:
• the liposome formulation is prepared through following steps:
• (i) dissolving the Wnt signal pathway inhibitor and β-cyclodextrin as a solubilizing agent in buffer solution of sodium dihydrogen phosphate at pH=5, vibrating overnight, removing supernatants by centrifugation to obtain saturated aqueous solution of the Wnt signal pathway inhibitor comprising 30% β-cyclodextrin;
• (ii) dissolving hydrogenated soybean lecithin, distearoyl phosphatidylethanolamine-polyethylene glycol and cholesterol in ethanol at a molar ratio of 55:5:40 to obtain ethanol solution of lipid molecules;
• (iii) adding ammonium sulfate solution containing 30% β-cyclodextrin to the ethanol solution of lipid molecules obtained in step (ii) to obtain blank vesicles, performing homogenization through MILLIPORE filtration membranes with pore sizes of 100 nm and 50 nm, and then performing dialysis using ammonium sulfate solution to remove ethanol from the blank vesicles and then performing dialysis using sodium dihydrogen phosphate to remove aqueous ammonium sulfate outside of the blank vesicles, thereby forming concentration gradient from interior to exterior of the blank vesicles;
• (iv) preheating the blank vesicles obtained in step (iii) at 60° C. for 10 min by immersing them into the constant temperature vibrator, then adding saturated aqueous solution of Wnt signal pathway inhibitor comprising 30% β-cyclodextrin obtained in step (i), vibrating at constant temperature, after incubating for a certain period, performing dialysis using 10% saccharose solution to remove free drug, thereby obtaining the liposome formulation with Wnt signal pathway inhibitor encapsulated therein.