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Magnetic liposomal emodin composite with enhanced killing efficiency against breast cancer

SongThese authors contributed equally to this work., Yonghong, Sheng, Zhujun, Xu, Yunjun, Dong, Liang, Xu, Weiping, Li, Fangyuan, Wang, Jing, Wu, Zeyu, Yang, Yi, Su, Yang, Sun, Xiaolian, Ling, Daishun, Lu, Yang
Biomaterials science 2019 v.7 no.3 pp. 867-875
Rheum palmatum, antineoplastic activity, biocompatibility, breast neoplasms, cytotoxicity, emodin, ferromagnetism, fluorescence, hemolysis, hydrophilicity, hydrophobicity, image analysis, ingredients, lipid bilayers, magnetic fields, mice, nanocomposites, nanomaterials, neoplasm cells, solubility, therapeutics
As an active natural ingredient extracted from the plant Rheum palmatum, emodin exhibits various pharmacological activities, especially the inhibition of tumor growth and migration. However, the anticancer activity of emodin is limited mainly due to its poor solubility and the lack of specific targeting. Herein, we employed liposome to load emodin into the lipid bilayer, and high-performance ferromagnetic iron oxide nanocubes were simultaneously encapsulated in the hydrophilic bilayer. The optimized magnetic liposomal emodin nanocomposite (MLE) exhibited a 24.1% increase in the efficiency of killing MCF-7 cancer cells at a low concentration of 16 μg mL⁻¹ compared with that of the hydrophobic free emodin. A further 8.67% enhancement of the killing efficiency was obtained by magnetic targeting. Benefitting from the high ferromagnetism, the transverse relaxivity (r₂) of MLE was measured to be as high as 392.9 mM⁻¹ s⁻¹. With guidance from the external magnetic field, the effective accumulation of this magnetic liposome in the tumor region of a 4T1 breast tumor bearing mouse was observed by both MR tracking and fluorescence imaging, which should be beneficial for decreasing the required therapeutic dose of emodin. Hemolysis, cytotoxicity and biochemistry assays confirmed the excellent biocompatibility of this magnetic liposomal carrier. The anti-tumor therapeutic effect of MLE was further investigated in vivo, and the tumor in the therapeutic group was almost eliminated, indicating that this magnetic liposomal emodin could serve as a novel magnetically guided theranostic nanoagent.