Yan Hongmei, Zhang Zhenhai, Jia Xiaobin, Song Jie
College of Pharmacy, Nanjing University of Chinese Medicine; Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Third School of Clinical Medical of Nanjing University of Chinese Medicine, Nanjing, People's Republic of China.
Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Third School of Clinical Medical of Nanjing University of Chinese Medicine, Nanjing, People's Republic of China.
Int J Nanomedicine. 2016 Sep 8;11:4563-4571. doi: 10.2147/IJN.S112204. eCollection 2016.
Baohuoside I, extracted from the Herba epimedii, is an effective but a poorly soluble antitumor drug. To improve its solubility, formulation of baohuoside I-loaded mixed micelles with d-α-tocopheryl polyethylene glycol succinate and Solutol HS 15 (BTSM) has been developed in this study. We performed a systematic comparative evaluation of the antiproliferative effect, cellular uptake, antitumor efficacy, and in vivo tumor targeting of these micelles using non-small-cell lung cancer (NSCLC) A549 cells. Results showed that the obtained micelles have a mean particle size of ~62.54 nm, and the size of micelles was narrowly distributed. With the improved cellular uptake, BTSM displayed a more potent anti-proliferative action on A549 cell lines than baohuoside I; half-maximal inhibitory concentration was 7.83 vs 20.37 µg/mL, respectively. The antitumor efficacy test in nude mice showed that BTSM exhibited significantly higher antitumor activity against NSCLC with lesser toxic effects on normal tissues. The imaging study for in vivo targeting demonstrated that the mixed micelles formulation achieved effective and targeted drug delivery. Therefore, BTSM might be a potential antitumor formulation.
淫羊藿苷 I 是从淫羊藿中提取的一种有效的抗肿瘤药物，但溶解性较差。为提高其溶解度，本研究开发了用聚乙二醇琥珀酸二-α-生育酚酯和 Solutol HS 15 制备载淫羊藿苷 I 的混合胶束（BTSM）。我们使用非小细胞肺癌（NSCLC）A549 细胞对这些胶束的抗增殖作用、细胞摄取、抗肿瘤疗效和体内肿瘤靶向性进行了系统的比较评估。结果表明，所制备的胶束平均粒径约为 62.54 nm，粒径分布较窄。随着细胞摄取的改善，BTSM 对 A549 细胞系的抗增殖作用比淫羊藿苷 I 更强；半数抑制浓度分别为 7.83 和 20.37 μg/mL。裸鼠抗肿瘤疗效试验表明，BTSM 对 NSCLC 表现出显著更高的抗肿瘤活性，对正常组织的毒性作用较小。体内靶向成像研究表明，混合胶束制剂实现了有效的靶向给药。因此，BTSM 可能是一种潜在的抗肿瘤制剂。
