Due to their various biological activities that are beneficial to human health and antitumor effect, flavonoid compounds have attracted much attention in recent years. Hydrous icaritin (HICT) was such a flavonoid that can inhibit the growth of breast cancer and cancer stem cells. In order to overcome the insolubility problem, HICT was fabricated into nanorods (NRs) through anti-solvent precipitation in this paper using D-α tocopherol acid polyethylene glycol succinate and sodium oleate as a co-stabilizer meanwhile using the mixture of ethanol and acetone (1:2, v/v) as the organic solvent. The obtained HICT NRs showed an average particle size 222.0 nm with a small polydispersity index value of 0.124 and a high zeta potential of - 49.5 mV. HICT NRs could maintain similar particle size in various physiological medium and could be directly lyophilized without the addition of any cytoprotectants and then reconstituted into a colloidal system of similar size. The resultant HICT NRs had a high drug loading content of 55.6% and released HICT in a steady and constant pattern. MTT assay indicated NRs enhanced HICT's antitumor activity to ninefold against MCF-7 breast carcinoma cells. In vivo studies demonstrated oral administration free HICT had almost no tumor inhibitory effect while HICT NRs showed a tumor inhibition rate of 47.8%. When intravenously injected, HICT NRs displayed similar therapeutic efficacy to paclitaxel injections (70.4% vs. 74.5%, TIR). This may be partly due to the high accumulation of the injected HICT NRs in tumor ranking only second to that in the liver but much higher than in other organs. These results demonstrated that HICT NRs could be a promising antitumor agent for the treatment of breast cancer in clinic.

中文翻译：

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具有优异稳定性的含水依卡里汀纳米棒改善了抗乳腺癌的体外和体内活性。

由于类黄酮化合物具有多种有益于人体健康和抗肿瘤作用的生物学活性，因此近年来受到了广泛的关注。含水icaritin（HICT）是一种类黄酮，可以抑制乳腺癌和癌症干细胞的生长。为了克服不溶性问题，本文使用D-α生育酚酸聚乙二醇琥珀酸酯和油酸钠作为助稳定剂，同时使用乙醇和丙酮的混合物通过反溶剂沉淀将HICT制成纳米棒（NR）。 1：2，v / v）作为有机溶剂。所获得的HICT NRs显示出平均粒径222.0 nm，具有小的多分散指数值0.124和高的ζ电位-49.5 mV。HICT NRs可以在各种生理介质中保持相似的粒径，并且可以直接冻干而无需添加任何细胞保护剂，然后重构为相似大小的胶体系统。所得的HICT NRs具有55.6％的高载药量，并以稳定且恒定的方式释放HICT。MTT分析表明，NRs将HICT对MCF-7乳腺癌细胞的抗肿瘤活性提高了9倍。体内研究表明，口服免费的HICT几乎没有抑制肿瘤的作用，而HICT NRs的抑制率为47.8％。当静脉注射时，HICT NRs显示出与紫杉醇注射剂相似的治疗效果（TIR为70.4％对74.5％）。这可能部分是由于注射的HICT NRs在肿瘤中的高积累，仅在肝脏中排名第二，但远高于其他器官。这些结果表明，HICT NRs可能是临床上有望用于乳腺癌治疗的抗肿瘤药物。