Hui Li1, Xiaoming Li2, Xinli Shi3, Zhen Li4, Yajing Sun4. 1. Postgraduate School, Hebei Medical University, Shijiazhuang, Hebei Province 050017, China; Department of Pathology, Bethune International Peace Hospital, Shijiazhuang, Hebei Province 050081, China. 2. Postgraduate School, Hebei Medical University, Shijiazhuang, Hebei Province 050017, China; Department of Otolaryngology Head and Neck Surgery, Bethune International Peace Hospital, Shijiazhuang, Hebei Province 050081, China. Electronic address: xmlmo@126.com. 3. Department of Basic Sciences, Hebei College of Traditional Chinese Medicine, Shijiazhuang, Hebei Province 050061, China. 4. Department of Otolaryngology Head and Neck Surgery, Bethune International Peace Hospital, Shijiazhuang, Hebei Province 050081, China.
Abstract
BACKGROUND: 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. PURPOSE: Magnetic DHA nano-liposomes (DHA-MLPs) were developed to improve the targeting antitumor efficiency and bioavailability of DHA, and their physical properties were characterized. STUDY DESIGN AND METHODS: 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. RESULTS: 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). CONCLUSION: 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.
BACKGROUND: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. PURPOSE: Magnetic DHA nano-liposomes (DHA-MLPs) were developed to improve the targeting antitumor efficiency and bioavailability of DHA, and their physical properties were characterized. STUDY DESIGN AND METHODS: 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. RESULTS: 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). CONCLUSION: 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.
Keywords:
Dihydroartemisinin; Head and neck squamous cell carcinoma; Liposomes; Magnetic dihydroartemisinin nano liposomes; Magnetic targeting; Nanoparticles