Novel tumor-targeting, self-assembling peptide nanofiber as a carrier for effective curcumin delivery.
Novel tumor-targeting, self-assembling peptide nanofiber as a carrier for effective curcumin delivery.
复制标题
新型肿瘤靶向自组装肽纳米纤维作为有效姜黄素递送的载体
DOI：
10.2147/ijn.s55875
复制
发表时间：
2014
影响因子：
8
通讯作者：
Yang C
中科院分区：
文献类型：
--
作者：
Liu J;Liu J;Xu H;Zhang Y;Chu L;Liu Q;Song N;Yang C
姜黄素较差的水溶性和较低的生物利用度限制了其在癌症治疗中的临床应用。在这项研究中，利用自组装的NAP-GFFYG-RGD多肽，开发了一种新型的肿瘤靶向纳米纤维载体，以改善姜黄素的溶解性和肿瘤靶向性。用透射电子显微镜观察了多肽纳米纤维和包覆姜黄素的纳米纤维的形态。以NAP-GFFYG-RGE多肽纳米纤维(f-RGE-CUR)为对照，研究了姜黄素包裹的NAP-GFFYG-RGD多肽纳米纤维(f-RGD-CUR)的体内外肿瘤靶向性。将姜黄素包裹在直径约为10-20 nm的多肽纳米纤维中。姜黄素在体外表现出纳米纤维的缓释行为。在αvβ3整合素阳性的肝癌细胞中，F-RGd-CUR的细胞摄取率明显高于非靶向f-RGE-CUR，从而导致显著更高的细胞毒作用。体外研究进一步证明，经尾静脉给药后，姜黄素可在小鼠肿瘤中显著蓄积。这些结果表明，NAP-GFFYG-RGD多肽自组装纳米纤维是一种很有前途的靶向治疗肿瘤的疏水给药系统。
The poor aqueous solubility and low bioavailability of curcumin restrict its clinical application for cancer treatment. In this study, a novel tumor-targeting nanofiber carrier was developed to improve the solubility and tumor-targeting ability of curcumin using a self-assembled Nap-GFFYG-RGD peptide. The morphologies of the peptide nanofiber and the curcumin-encapsulated nanofiber were visualized by transmission electron microscopy. The tumor-targeting activity of the curcumin-encapsulated Nap-GFFYG-RGD peptide nanofiber (f-RGD-Cur) was studied in vitro and in vivo, using Nap-GFFYG-RGE peptide nanofiber (f-RGE-Cur) as the control. Curcumin was encapsulated into the peptide nanofiber, which had a diameter of approximately 10–20 nm. Curcumin showed sustained-release behavior from the nanofibers in vitro. f-RGD-Cur showed much higher cellular uptake in αvβ3 integrin-positive HepG2 liver carcinoma cells than did non-targeted f-RGE-Cur, thereby leading to significantly higher cytotoxicity. Ex vivo studies further demonstrated that curcumin could accumulate markedly in mouse tumors after administration of f-RGD-Cur via the tail vein. These results indicate that Nap-GFFYG-RGD peptide self-assembled nanofibers are a promising hydrophobic drug delivery system for targeted treatment of cancer.