1. β-Elemene-loaded polymeric micelles intensify anti-carcinoma efficacy and alleviate side effects
- Author
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Zejiang Zhu, Caixia Dou, Lijuan Chen, Qiaoqiao Hu, Peng Bai, Rongsheng Tong, Zhengying Su, Lulu Cai, Bai Lan, Junfeng Yan, Wuyu Zhang, and Minghai Tang
- Subjects
Tube formation ,Drug ,Chemistry ,media_common.quotation_subject ,02 engineering and technology ,General Chemistry ,Pharmacology ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,Micelle ,0104 chemical sciences ,Bioavailability ,chemistry.chemical_compound ,Pharmacokinetics ,Drug delivery ,Toxicity ,0210 nano-technology ,Elemene ,media_common - Abstract
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 T1/2 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.
- Published
- 2020
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