Zhong Tao, He Bin, Cao Hai-Qiang, Tan Tao, Hu Hai-Yan, Li Ya-Ping, Zhang Zhi-Wen
College of Pharmacy, Nanchang University, Nanchang 330006, China.
State Key Laboratory of Drug Research &Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Acta Pharmacol Sin. 2017 Jun;38(6):924-930. doi: 10.1038/aps.2017.36. Epub 2017 May 1.
Cancer metastasis is the primary cause of high mortality in breast cancer patients. In this study, we loaded an anti-cancer drug, cabazitaxel (CTX), into polymeric micelles (CTX-loaded polymeric micelles, PCMs), and explored their therapeutic efficacy in breast cancer metastasis. The characteristics of PCMs were investigated, and their anti-metastatic efficacy was assessed using in vitro and in vivo evaluations. PCMs had an average diameter of 50.13±11.96 nm with a CTX encapsulation efficiency of 97.02%±0.97%. PCMs could be effectively internalized into metastatic 4T1 breast cancer cells in vitro. CTX (10 ng/mL) or an equivalent concentration in PCMs did not significantly affected the viability of 4T1 cells, but dramatically decreased the cell migration activities. In an orthotopic metastatic breast cancer model, intravenously administered PCMs could be efficiently delivered to the tumor sites, resulting in a 71.6% inhibition of tumor growth and a 93.5% reduction of lung metastases. Taken together, our results verify the anti-metastatic efficacy of PCMs, thus providing an encouraging strategy for treating breast cancer metastasis.
癌症转移是乳腺癌患者高死亡率的主要原因。在本研究中，我们将一种抗癌药物卡巴他赛（CTX）载入聚合物胶束（载CTX聚合物胶束，PCMs）中，并探究了它们对乳腺癌转移的治疗效果。对PCMs的特性进行了研究，并通过体外和体内评估来评价其抗转移疗效。PCMs的平均直径为50.13±11.96 nm，CTX包封率为97.02%±0.97%。体外实验中，PCMs能有效被转移性4T1乳腺癌细胞内化。CTX（10 ng/mL）或PCMs中同等浓度的CTX对4T1细胞活力无显著影响，但显著降低了细胞迁移活性。在原位转移性乳腺癌模型中，静脉注射的PCMs能有效递送至肿瘤部位，导致肿瘤生长抑制率达71.6%，肺转移减少93.5%。综上所述，我们的结果证实了PCMs的抗转移疗效，从而为治疗乳腺癌转移提供了一种令人鼓舞的策略。
