Materials Science & Engineering C, 2016, 59:792-800.

Genistein-loaded nanoparticles of star-shaped diblock copolymer mannitol core PLGA-TPGS for the treatment of liver cancer

Binquan Wu, Yong Liang, Yi Tan, et al

Department of Hepatobiliary Surgery, The First Affiliated Hospital of Bengbu Medical College, Bengbu 233004, China; et al

The purpose of this research is to develop nanoparticles (NPs) of star-shaped copolymer mannitol-functionalized PLGA-TPGS for Genistein delivery for liver cancer treatment, and evaluate their therapeutic effects in liver cancer cell line and hepatoma-tumor-bearing nude mice in comparison with the linear PLGA nanoparticles and PLGA-TPGS nanoparticles. The Genistein-loaded M-PLGA-TPGS nanoparticles (MPTN), prepared by a modified nanoprecipitation method, were observed by FESEM and TEM to be near-spherical shape with narrow size distribution. The nanoparticles were further characterized in terms of their size, size distribution, surface charge, drug-loading content, encapsulation efficiency and in vitro drug release profiles. The data showed that the M-PLGA-TPGS nanoparticles were found to be stable, showing almost no change in particle size and surface charge during 3-month storage of their aqueous solution. In vitro Genistein release from the nanoparticles exhibited biphasic pattern with burst release at the initial 4days and sustained release afterwards. The cellular uptake efficiency of fluorescent M-PLGA-TPGS nanoparticles was 1.25-, 1.22-, and 1.29-fold higher than that of the PLGA-TPGS nanoparticles at the nanoparticle concentrations of 100, 250, and 500μg/mL, respectively. In the MPTN group, the ratio of apoptotic cells increased with the drug dose increased, which exhibited dose-dependent effect and a significant difference compared with Genistein solution group (p<0.05). The data also showed that the Genistein-loaded M-PLGA-TPGS nanoparticles have higher antitumor efficacy than that of linear PLGA-TPGS nanoparticles and PLGA nanoparticles in vitro and in vivo. In conclusion, the star-shaped copolymer M-PLGA-TPGS could be used as a potential and promising bioactive material for nanomedicine development for liver cancer treatment.

中国《材料科学与工程》, 2016, 59:792-800.

星型嵌段共聚物甘露醇的核心PLGA-TPGS负载染料木黄酮的纳米颗粒用于治疗肝细胞癌

吴彬全，梁勇，谭易，等

蚌埠医学院第一附属医院肝胆外科，蚌埠233004; et al

本研究的目的是要开发纳米 (NPs) 的星状共聚物甘露醇-官能化 PLGA TPGS 肝癌治疗的金雀异黄素交付和评估其疗效在肝癌细胞株和肝癌荷瘤裸小鼠与线性 PLGA 纳米粒和 TPGS PLGA 纳米粒。金雀异黄素加载 TPGS-M-PLGA 纳米粒 (MPTN)，改性的沉淀法制备观察 FESEM 和透射电镜是近球形形状尺寸分布窄。其大小、 粒度分布和表面电荷进一步表征了纳米粒子、 载药量含量、 包封率和体外药物释放曲线。数据表明，M-PLGA-TPGS 纳米粒子稳定，其水溶液 3 月贮藏过程中粒子的大小和表面电荷显示几乎没有变化。从纳米粒的体外金雀异黄素释放之后展出在最初的 4 个工作日的突释和缓释两相模式。M-PLGA-TPGS 荧光纳米颗粒的细胞吸收效率是 1.25-1.22-和 1.29-fold 高于 TPGS PLGA 纳米颗粒在纳米粒子浓度的 100、 250 和 500μg/mL，分别。在 MPTN 组中，细胞凋亡率增加药物剂量的增加，其中展出的剂量依赖效应与金雀异黄素解决方案组相比显著差异 (p < 0.05)。数据还显示，金雀异黄素加载 TPGS-M-PLGA 纳米粒有更高的抗肿瘤功效比线性 TPGS PLGA 纳米粒与 PLGA 纳米粒的体外和体内。总之，星状共聚物 M PLGA TPGS 可以用作治疗原发性肝癌纳米医学发展的潜力和良好的生物活性物质。