School of Pharmacy, Nantong University, 19 Qixiu Road, Nantong 226001, Jiangsu, China.
School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, Liaoning, China.
Molecules. 2018 Oct 25;23(11):2760. doi: 10.3390/molecules23112760.
Multi-drug resistance (MDR) presents a serious problem in cancer chemotherapy. In this study, Vitamin E (VE)-Albumin core-shell nanoparticles were developed for paclitaxel (PTX) delivery to improve the chemotherapy efficacy in an MDR breast cancer model. The PTX-loaded VE-Albumin core-shell nanoparticles (PTX-VE NPs) had small particle sizes (about 100 nm), high drug entrapment efficiency (95.7%) and loading capacity (12.5%), and showed sustained release profiles, in vitro. Docking studies indicated that the hydrophobic interaction and hydrogen bonds play a significant role in the formation of the PTX-VE NPs. The results of confocal laser scanning microscopy analysis demonstrated that the cell uptake of PTX was significantly increased by the PTX-VE NPs, compared with the NPs without VE (PTX NPs). The PTX-VE NPs also exhibited stronger cytotoxicity, compared with PTX NPs with an increased accumulation of PTX in the MCF-7/ADR cells. Importantly, the PTX-VE NPs showed a higher anti-cancer efficacy in MCF-7/ADR tumor xenograft model than the PTX NPs and the PTX solutions. Overall, the VE-Albumin core-shell nanoparticles could be a promising nanocarrier for PTX delivery to improve the chemotherapeutic efficacy of MDR cancer.
多药耐药性（MDR）是癌症化疗中的一个严重问题。在本研究中，开发了维生素 E（VE）-白蛋白核壳纳米粒用于紫杉醇（PTX）递送，以提高 MDR 乳腺癌模型中的化疗疗效。载紫杉醇的 VE-白蛋白核壳纳米粒（PTX-VE NPs）具有较小的粒径（约 100nm）、高药物包封效率（95.7%）和载药能力（12.5%），并表现出体外持续释放的特性。对接研究表明，疏水性相互作用和氢键在 PTX-VE NPs 的形成中起着重要作用。共聚焦激光扫描显微镜分析的结果表明，与不含 VE 的 NPs（PTX NPs）相比，PTX-VE NPs 显著增加了 PTX 的细胞摄取。PTX-VE NPs 还表现出更强的细胞毒性，与在 MCF-7/ADR 细胞中增加 PTX 积累的 PTX NPs 相比。重要的是，PTX-VE NPs 在 MCF-7/ADR 肿瘤异种移植模型中的抗癌疗效高于 PTX NPs 和 PTX 溶液。总体而言，VE-白蛋白核壳纳米粒可以作为一种有前途的 PTX 递送纳米载体，以提高 MDR 癌症的化疗疗效。
