Curcumin loaded polymeric micelles inhibit breast tumor growth and spontaneous pulmonary metastasis
Curcumin loaded polymeric micelles inhibit breast tumor growth and spontaneous pulmonary metastasis
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姜黄素负载的聚合物胶束抑制乳腺肿瘤生长和自发性肺转移
DOI：
10.1016/j.ijpharm.2012.12.032
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发表时间：
2013-02-25
影响因子：
5.8
通讯作者：
Wei, Yuquan
中科院分区：
文献类型：
--
作者：
Liu, Lei;Sun, Lu;Wei, Yuquan
本研究旨在开发姜黄素（Cur）负载的可生物降解自组装聚合物胶束（Cur- m），以克服姜黄素的水溶性差和满足静脉给药的要求。采用固体分散法制备cu - m，工艺简单，易于规模化生产。cu - m的粒径为28.2 +/- 1.8 nm，多分散指数（PDI）为0.136 +/- 0.050，载药量和包封效率分别为14.84 +/- 0.11%和98.91 +/- 0.70%。此外，游离Cur的快速释放与cu - m的缓释有显著差异。细胞毒性研究表明，包封后的Cur仍具有较强的抗肿瘤作用。此外，在4T1乳腺癌皮下肿瘤模型中，Cur-M能更有效地抑制肿瘤生长和自发肺转移，延长荷瘤小鼠的生存期。此外，免疫荧光和免疫组织化学研究也表明，curm处理小鼠肿瘤中凋亡细胞增多，微血管减少，增殖阳性细胞减少。综上所述，聚合胶束包埋的Cur对乳腺肿瘤具有较强的抗肿瘤和抗转移活性，Cur- m是一种优良的水基Cur制剂，可能成为乳腺癌治疗的候选药物。(C) 2012 Elsevier B.V.版权所有
This work aims to develop curcumin (Cur) loaded biodegradable self-assembled polymeric micelles (Cur-M) to overcome poor water solubility of Cur and to meet the requirement of intravenous administration. Cur-M were prepared by solid dispersion method, which was simple and easy to scale up. Cur-M had a small particle size of 28.2 +/- 1.8 nm and polydisperse index (PDI) of 0.136 +/- 0.050, and drug loading and encapsulation efficiency of Cur-M were 14.84 +/- 0.11% and 98.91 +/- 0.70%, respectively. Besides, in vitro release profile showed a significant difference between rapid release of free Cur and much slower and sustained release of Cur-M. Cytotoxicity study showed that the encapsulated Cur remained its potent anti-tumor effect. Furthermore, Cur-M were more effective in inhibiting tumor growth and spontaneous pulmonary metastasis in subcutaneous 4T1 breast tumor model, and prolonged survival of tumor-bearing mice. In addition, immunofluorescent and immunohistochemical studies also showed that tumors of Cur-M- treated mice had more apoptosis cells, fewer microvessels, and fewer proliferation-positive cells. In conclusion, polymeric micelles encapsulating Cur were developed with enhanced anti-tumor and antimetastasis activity on breast tumor, and Cur-M is excellent water-based formulation of Cur which may serve as a candidate for breast cancer therapy. (C) 2012 Elsevier B.V. All rights reserved.