脂质体
双氢青蒿素
体内
化学
体外
细胞凋亡
药理学
医学
生物化学
生物
免疫学
青蒿素
生物技术
疟疾
恶性疟原虫
作者
Hui Li,Xiaoming Li,Xinli Shi,Zhen Li,Yajing Sun
出处
期刊:Phytomedicine
[Elsevier]
日期:2018-11-06
卷期号:56: 215-228
被引量:35
标识
DOI:10.1016/j.phymed.2018.11.007
摘要
Dihydroartemisinin (DHA) was one of the most potent anticancer artemisinin-like compounds that had been proved by many researchers, but its application was limited by its own characteristics. Magnetic DHA nano-liposomes (DHA-MLPs) were developed to improve the targeting antitumor efficiency and bioavailability of DHA, and their physical properties were characterized. Liposomes were prepared by thin film dispersion and orthogonal experimental design was used to optimize the formula. The magnetic targeting and antitumor effects of DHA-MLPs in the externally applied magnetic field was investigated in vitro and in vivo. The mean particle size of DHA-MLPs was 209.10 ± 4.92 nm, the charge potential was -37.13 ± 1.01 mV, the encapsulation efficiency (E.E.%) was 82.12 ± 0.91%, and the saturation magnetization at room temperature was 11.84 emu g−1. Targeting DHA-MLPs as well as free DHA could lead to cell cycle G1 block and apoptosis of HNSCC tumor cells in vitro. The tumor volumes of targeting DHA-MLPs treated mouse group were distinctly decreased than that in the control group, free DHA group and non-targeting DHA-MLPs group (P < 0.05). It was observed from iron staining intensity that DHA-MLPs had significant targeting effect in magnetic field (P < 0.05). This novelty liposome could strengthen the ability of DHA in tumor suppression, by increasing the targeted delivery of DHA and biocompatibility, optimize the bioefficacy of DHA.
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