Biodegradable micelles enhance the antiglioma activity of curcumin in vitro and in vivo.
Biodegradable micelles enhance the antiglioma activity of curcumin in vitro and in vivo.
复制标题
可生物降解的胶束增强姜黄素的体外和体内抗神经胶质瘤活性
DOI：
10.2147/ijn.s102450
复制
发表时间：
2016
影响因子：
8
通讯作者：
You C
中科院分区：
文献类型：
--
作者：
Zheng S;Gao X;Liu X;Yu T;Zheng T;Wang Y;You C
姜黄素（Curcumin，Cur）是姜黄（Curcumalonga）中的一种天然多酚，具有抗肿瘤活性。然而，由于其水溶性差，生物利用度低，临床应用相当有限。将疏水性药物包裹在纳米粒中是提高药物活性的有效途径。在本研究中，通过自组装的方法与可生物降解的单甲氧基聚乙二醇-聚乳酸共聚物（MPEG-PLA）的纳米胶束负载Cur。包封后，细胞摄取增加，并且Cur可以以持续的方式从MPEG-PLA胶束中释放。Cur/MPEG-PLA胶束（Cur/MPEG-PLA胶束）对C6和U251胶质瘤细胞的毒性增强，并诱导C6胶质瘤细胞凋亡。此外，Cur/MPEG-PLA胶束的治疗效率进行了评估，在负载胶质瘤的裸鼠模型的长度。Cur/MPEG-PLA胶束对肿瘤生长的抑制作用优于Cur，表明Cur/MPEG-PLA胶束增强了Cur的体内抗胶质瘤活性。免疫组化和免疫荧光分析结果表明，诱导细胞凋亡，抑制血管生成，抑制细胞增殖可能有助于提高抗胶质瘤作用。提示Cur/MPEG-PLA在脑胶质瘤治疗中具有潜在的临床应用价值。
Curcumin (Cur), a natural polyphenol of Curcuma longa, has been recently reported to possess antitumor activities. However, due to its poor aqueous solubility and low biological availability, the clinical application of Cur is quite limited. The encapsulation of hydrophobic drugs into nanoparticles is an effective way to improve their pharmaceutical activities. In this research, nanomicelles loaded with Cur were formulated by a self-assembly method with biodegradable monomethoxy poly(ethylene glycol)-poly(lactide) copolymers (MPEG-PLAs). After encapsulation, the cellular uptake was increased and Cur could be released from MPEG-PLA micelles in a sustained manner. The Cur-loaded MPEG-PLA micelles (Cur/MPEG-PLA micelles) exhibited an enhanced toxicity on C6 and U251 glioma cells and induced more apoptosis on C6 glioma cells compared with free Cur. Moreover, the therapy efficiency of Cur/MPEG-PLA micelles was evaluated at length on a nude mouse model bearing glioma. The Cur/MPEG-PLA micelles were more effective on suppressing tumor growth compared with free Cur, which indicated that Cur/MPEG-PLA micelles improved the antiglioma activity of Cur in vivo. The results of immunohistochemical and immunofluorescent analysis indicated that the induction of apoptosis, antiangiogenesis, and inhibition of cell proliferation may contribute to the improvement in antiglioma effects. Our data suggested that Cur/MPEG-PLA may have potential clinic applications in glioma therapy.