AbstractCurcumol (Cur), which is the primary active anti‐liver cancer component of Chinese traditional medicine Rhizoma zedoariae, was encapsulated in galactosylated liposomes to enhance its liver‐targeting efficacy. In this study, we optimized the preparation methods, prescription, and process of galactosylated curcumol liposomes (Gal‐Cur‐L). The experimental results showed that the encapsulation efficiency, particle diameter, and stability coefficient of Gal‐Cur‐L obtained by the two‐step emulsification method were improved compared with those of it obtained by other methods. Single‐factor investigation showed that two factors, pH and the amount of triolein, contribute at least partly to the encapsulation efficiency and particle diameter of Gal‐Cur‐L. The best prescription and process were obtained through orthogonal test: the ratio of lecithin to cholesterol was 2:1, the ratio of drug to lipid was 1:2, and the amount of ether and Twain‐80 were 4 ml and 1.6 g/L, respectively, 15 min for ultrasonic time, 100 W for ultrasonic power, and 20 min for homogeneous time. Using the best method, prescription, and process mentioned earlier, the basic test results of Gal‐Cur‐L were obtained, which demonstrated that our methods, prescription, and process of Gal‐Cur‐L were applicable. The encouraging results of this study provided references for the research of liver‐targeting reagents of curcumol.
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