Citation: Hu Qiaoqiao, Bai Lan, Zhu Zejiang, Su Zhengying, Bai Peng, Tang Minghai, Dou Caixia, Yan Junfeng, Tong Rongsheng, Zhang Wuyu, Chen Lijuan, Cai Lulu. β-Elemene-loaded polymeric micelles intensify anti-carcinoma efficacy and alleviate side effects[J]. Chinese Chemical Letters, ;2020, 31(3): 915-918. doi: 10.1016/j.cclet.2020.01.008 shu

β-Elemene-loaded polymeric micelles intensify anti-carcinoma efficacy and alleviate side effects

Hu Qiaoqiao ^a,1 ,
Bai Lan ^a,1 ,
Zhu Zejiang ^b ,
Su Zhengying ^b ,
Bai Peng ^b ,
Tang Minghai ^b ,
Dou Caixia ^b ,
Yan Junfeng ^a ,
Tong Rongsheng ^a ,
Zhang Wuyu ^c ,
Chen Lijuan ^b,*, ,
Cai Lulu ^a,*,

a.
Personalized Drug Therapy Key Laboratory of Sichuan Province, Department of Pharmacy, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610072, China
b.
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu 610041, China
c.
Department of Chemistry, University of Louisville, Louisville, KY 40292, United States

chenlijuan125@163.com

cailulu@med.uestc.edu.cn

Received Date: 8 November 2019
Revised Date: 3 January 2020
Accepted Date: 3 January 2020
Available Online: 7 January 2020

Figures(5)

β-Elemene is a volatile oil used for the treatment of cancer, but poor solubility, low bioavailability, and various adverse reactions limit its application. For ameliorating risks of the venous toxicity of β-elemene, intravenously injectable micelle of β-elemene was prepared using the thin-film hydration method. The results pointed out the micelles were uniformly spherical with about 20.96 ± 0.1966 nm in average diameter and exhibited high entrapment efficiency (99.02% ± 0.88%). As revealed by drug release studies in vitro, β-elemene micelles had sustained drug release. Compared with free β-elemene, the micelles increased the drug cellular uptake and enhanced the anti-tumor effect in vitro through retarding cell cycle and inducing apoptosis. Meanwhile, the elevated serum stability of β-elemene micelles implied less drug leakage and reduced toxicity. The wound healing and tube formation assay in vitro demonstrated the anti-metastasis and anti-angiogenesis effects of β-elemene micelles. Moreover, the pharmacokinetics study showed the AUC and T_1/2 of β-elemene in micelle group were 1.79 and 1.62 times of that in free β-elemene group, suggesting the circulation time of β-elemene in the blood had been prolonged. In addition, β-elemene micelles showed a favorable antitumor response compared with the β-elemene solution on C26 colon cancer-bearing mice model. Local irritation study investigated in rabbits indicated that the β-elemene micelles strikingly mitigated the irritation to the injection sites compared with free β-elemene. These results proved that the micelle could be a good candidate as an auspicious drug delivery system of β-elemene for the prospective clinical treatment of carcinoma.
- β-Elemene,
- mPEG-PCL micelles,
- Antitumor,
- Colon cancer,
- Irritation
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