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Preparation and Evaluation of Artemether Liposomes for Enhanced Anti-Tumor Therapy

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Abstracts

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 t1/2β, 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.

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Acknowledgements

The authors would like to express thanks to the School of Pharmaceutical Science, Shandong University, for providing the required infrastructure to carry the research. The authors thank their classmates in the same laboratory for their assistance.

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Authors and Affiliations

  1. School of Pharmaceutical Sciences, Shandong University, 44 Wenhua Xi Road, Ji’nan, 250012, Shandong Province, People’s Republic of China

    Liu Tian, Jingjing Liu, Zhenlei Yang & Guihua Huang

  2. Shandong Academy of Pharmaceutical Sciences, 989 Xinluo Street, Ji’nan, 250012, China

    Qingwen Jia & Yong Ying

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  1. Liu Tian
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  2. Jingjing Liu
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  3. Qingwen Jia
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  4. Yong Ying
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  5. Zhenlei Yang
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  6. Guihua Huang
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Correspondence to Guihua Huang.

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The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.

Ethical Approval

The animal experiment protocol was reviewed and approved by the Institutional Animal Care and Use Committee of Shandong University.

This article does not contain any studies with human participants performed by any of the authors.

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Tian, L., Liu, J., Jia, Q. et al. Preparation and Evaluation of Artemether Liposomes for Enhanced Anti-Tumor Therapy. AAPS PharmSciTech 19, 512–521 (2018). https://doi.org/10.1208/s12249-017-0896-9

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  • DOI: https://doi.org/10.1208/s12249-017-0896-9

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