标题：Preparation and Evaluation of Artemether Liposomes for Enhanced Anti-Tumor Therapy
作者：Tian, Liu; Liu, Jingjing; Jia, Qingwen; Ying, Yong; Yang, Zhenlei; Huang, Guihua
作者机构：[Tian, Liu; Liu, Jingjing; Yang, Zhenlei; Huang, Guihua] Shandong Univ, Sch Pharmaceut Sci, 44 Wenhua Xi Rd, Jinan 250012, Shandong, Peoples R China.; 更多
通讯作者地址：[Huang, GH]Shandong Univ, Sch Pharmaceut Sci, 44 Wenhua Xi Rd, Jinan 250012, Shandong, Peoples R China.
关键词：artemether; liposomes; anti-tumor; pharmacokinetics; pharmacodynamics
摘要：The aim of the study was to design liposomes (Lips) of artemether (ARM), a plant-derived drug for treatment of metastatic tumors, for the intravenous delivery. The ARM-Lips were prepared using ethanol injection method. Based on the optimization of formulation with single-factor experiments, ARM-Lips were spherical with a uniform particle size (187.3 +/- 1.83) nm and its EE and DL were (94.49 +/- 1.18)% and (10.94 +/- 0.10)%, respectively. The in vitro drug release characteristics of ARM-Lips possessed a sustained release characteristic, and their behavior was in accordance with the first-order kinetics equation. In vivo, after intravenous injection to mice, the t1/2 beta, MRT, and AUC of ARM-Lips were 8.38-, 3.38-, and 3.11-fold those of ARM solution (ARM-Sol), respectively. In the pharmacodynamics studies, the tumor doubling time, growth inhibition rate, and specific growth rate of tumor of ARM-Lips were 1.97 times, 1.54 times, and 0.51 times those of ARM-Sol, respectively, which indicated that the anti-tumor effect of ARM-Lips was significantly stronger than that of ARM-Sol. These encouraging results revealed that ARM-Lips would serve as an efficient carrier for ARM for increasing therapeutic efficacy on tumor.