a Department of Pharmaceutical Sciences, School of Pharmacy , Shanghai University of Traditional Chinese Medicine , Shanghai , China.
Artif Cells Nanomed Biotechnol. 2018;46(sup2):921-935. doi: 10.1080/21691401.2018.1473412. Epub 2018 May 23.
The antitumor applications of curcumin (CUR) are limited because of its low water solubility, poor stability, and low bioavailability. We developed novel nanocarrier systems for tumour targeting and controlled CUR release and evaluated their therapeutic efficacy.
The surface of mesoporous silica nanoparticles (MSN) was modified with hyaluronan (HA) or polyethyleneimine-folic acid (PEI-FA) via disulfide bonds. The capacity of the resultant nanocarriers (MSN-HA and MSN-PEI-FA, respectively) for CUR delivery was evaluated in a breast cancer cell line and a mouse xenograft model.
MSN/CUR-PEI-FA and MSN/CUR-HA were cytotoxic to MDA-MB-231 breast cancer cells. Both formulations showed an enhanced cellular uptake compared with that of a non-targeted nanocarrier, with a greater cellular uptake of FA-modified nanoparticles than that of HA-modified nanoparticles. Accordingly, MSN-PEI-FA showed more precise targeting and higher accumulation in tumours than did MSN-HA, as visualized by live imaging. Both types of nanoparticles had good biocompatibility and low toxicity, and MSN/CUR-PEI-FA inhibited the tumour growth to a greater degree than did free CUR. Thus, MSN/CUR-PEI-FA are a promising drug delivery system for the treatment of breast cancer.
姜黄素 (CUR) 的抗肿瘤应用受到其低水溶性、差稳定性和低生物利用度的限制。我们开发了用于肿瘤靶向和控制 CUR 释放的新型纳米载体系统，并评估了它们的治疗效果。
通过二硫键将透明质酸 (HA) 或聚乙烯亚胺-叶酸 (PEI-FA) 修饰到介孔硅纳米颗粒 (MSN) 的表面。在乳腺癌细胞系和小鼠异种移植模型中评估所得纳米载体 (MSN-HA 和 MSN-PEI-FA) 对 CUR 递送的能力。
MSN/CUR-PEI-FA 和 MSN/CUR-HA 对 MDA-MB-231 乳腺癌细胞具有细胞毒性。与非靶向纳米载体相比，这两种制剂均显示出增强的细胞摄取，FA 修饰的纳米粒子的细胞摄取大于 HA 修饰的纳米粒子。因此，通过活体成像观察到，MSN-PEI-FA 比 MSN-HA 具有更精确的靶向性和更高的肿瘤积累。两种类型的纳米粒子均具有良好的生物相容性和低毒性，并且 MSN/CUR-PEI-FA 抑制肿瘤生长的程度大于游离 CUR。因此，MSN/CUR-PEI-FA 是治疗乳腺癌的有前途的药物递送系统。
