Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, 518055, China.
Department of Chemistry, Tsinghua University, Beijing, 100084, China.
Small. 2017 Aug;13(29). doi: 10.1002/smll.201700623. Epub 2017 Jun 8.
A nanocarrier system of d-a-tocopheryl polyethylene glycol 1000 succinate (TPGS)-functionalized polydopamine-coated mesoporous silica nanoparticles (NPs) is developed for sustainable and pH-responsive delivery of doxorubicin (DOX) as a model drug for the treatment of drug-resistant nonsmall cell lung cancer. Such nanoparticles are of desired particle size, drug loading, and drug release profile. The surface morphology, surface charge, and surface chemical properties are also successfully characterized by a series of techniques such as transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS), Brunauer-Emmett-Teller (BET) method, thermal gravimetric analysis (TGA), dynamic light scattering (DLS), and Fourier transform infrared spectroscopy (FTIR). The normal A549 cells and drug-resistant A549 cells are employed to access the cytotoxicity and cellular uptake of the NPs. The therapeutic effects of TPGS-conjugated nanoparticles are evaluated in vitro and in vivo. Compared with free DOX and DOX-loaded NPs without TPGS ligand modification, MSNs-DOX@PDA-TPGS exhibits outstanding capacity to overcome multidrug resistance and shows better in vivo therapeutic efficacy. This splendid drug delivery platform can also be sued to deliver other hydrophilic and hydrophobic drugs.
一种 d-a-生育酚聚乙二醇 1000 琥珀酸酯（TPGS）功能化聚多巴胺包覆介孔硅纳米粒子（NPs）的纳米载体系统被开发用于可持续和 pH 响应的阿霉素（DOX）递送，DOX 作为治疗耐药非小细胞肺癌的模型药物。这些纳米粒子具有所需的粒径、载药量和药物释放特性。通过一系列技术，如透射电子显微镜（TEM）、X 射线光电子能谱（XPS）、BET 方法、热重分析（TGA）、动态光散射（DLS）和傅里叶变换红外光谱（FTIR），成功地对其表面形态、表面电荷和表面化学性质进行了表征。正常的 A549 细胞和耐药的 A549 细胞被用于评估 NPs 的细胞毒性和细胞摄取。TPGS 缀合纳米粒子的治疗效果在体外和体内进行了评估。与游离 DOX 和没有 TPGS 配体修饰的载 DOX NPs 相比，MSNs-DOX@PDA-TPGS 表现出出色的克服多药耐药的能力，并显示出更好的体内治疗效果。这个出色的药物递送平台还可以用于输送其他亲水性和疏水性药物。
