Jing-Yi CHEN, Xiang REN, Li CHEN, Qian PENG, Jing-Yang LI, Ling ZHANG, Jin-Ning ZHANG, Xiao-Hui WANG, Fu-Duan LIU; Li ZHAN. Lung-Targeting Asiaticoside-Loaded Cationic Liposomes for Injection; Advanced Nano-Bio-Materials and Devices; 2017:1(4):210-222


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This study aimed to develop a sustained-releasing asiaticoside-loaded liposome with well lung-targeting. Liposomes were prepared by film-dispersion and extrusion method. The rotatable central composite design (RCCD) with three-factor and five-level were applied to evaluate the optimization experiments. To maximize the percentage encapsulation efficiency (EE) and drug loading, a quadratic polynomial model was generated to predict and evaluate the independent variables with respect to the dependent variables. Fitting RCCD model were confirmed by the ANOVA Table (P<0.05) through variance analysis, which predicted values of EE (%) and drug loading in good agreement with experimental values. By solving the regression equation and analyzing the response surface, the optimal result for the preparation of D-mannose modified asiaticoside-loaded liposomes, three-dimensional model graphs and plots, were found as follows: the ratio of drug to lipid is 0.07;the ratio of cholesterol to drug is 0.17;and the content of D-mannose is 0.03 g·ml-1. The encapsulation efficiency was 75.529±1.071 % (n=3), the drug loading was 2.539±0.029% (n=3) and the deviation from the predicted values were -0.217% and 0.205%,respectively. The release profiles, pharmacokinetic behaviors and tissue uptake were performed. The results indicated that the asiaticoside loaded in liposomes could have slow and well-controlled release, and half-life increased obviously in vivo. Meanwhile, the asiaticoside would focus on the lung when the octadecylamine was conjugated on the surface of liposomes.