Oral Nanomedicine Based on Multicomponent Microemulsions for Drug-Resistant Breast Cancer Treatment
Oral Nanomedicine Based on Multicomponent Microemulsions for Drug-Resistant Breast Cancer Treatment
复制标题
基于多组分微乳的口服纳米药物治疗耐药乳腺癌
DOI：
10.1021/acs.biomac.7b00011
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发表时间：
2017-04-01
影响因子：
6.2
通讯作者：
Mo, Ran
中科院分区：
文献类型：
--
作者：
Qu, Ding;Wang, Lixiang;Mo, Ran
本研究的目的是利用多组分微乳（ECG-MEs）作为口服给药系统来证明抗癌药物对耐药乳腺癌的治疗效果。依托oposide负载的ECG-MEs由薏苡仁油和人参皂苷Rh2 （G-Rh2）组成，两者不仅具有与依托oposide协同抗肿瘤的作用，而且具有类似赋形剂的特性。经口服给药的ECG-MEs被证明能够作为完整的载体穿过肠道进入血液循环后在肿瘤部位积聚。ECG-MEs的时空控制释放特性导致初始释放的G-Rh2对P-gp具有有效的抑制作用，并增加了顺序释放的依托苷在细胞内的积累。采用ECG-MEs验证依托泊苷、G-Rh2和薏苡仁油联合抗肿瘤活性。此外，安全性评估研究表明，用ECG-MEs治疗在体内没有引起任何显著的毒性。这些发现表明，ECG-MEs作为一种口服制剂可能为治疗耐药乳腺癌提供一种有希望的策略。
The aim of this study is to demonstrate the enhanced therapeutic efficacy of anticancer drugs on drug-resistant breast cancer using multicomponent microemulsions (ECG-MEs) as an oral delivery system. The etoposide-loaded ECG-MEs were composed of coix seed oil and ginsenoside Rh2 (G-Rh2), both of which possess not only the synergistic antitumor effect with etoposide, but also have excipient-like properties. Orally administrated ECG-MEs were demonstrated to be able to accumulate at the tumor site following crossing the intestines as intact vehicles into the blood circulation. The spatiotemporal controlled release characteristics of ECG-MEs brought about the efficient P-gp inhibition by the initially released G-Rh2 and the increased intracellular accumulation of the sequentially released etoposide. The combination antitumor activity of etoposide, G-Rh2 and coix seed oil using ECG-MEs was verified on the xenograft drug-resistant breast tumor mouse models. In addition, the safety evaluation studies indicated that treatment with ECG-MEs did not cause any significant toxicity in vivo. These findings suggest that ECG-MEs as an oral formulation may offer a promising strategy to treat the drug-resistant breast cancer.