Bacillus-Shape Design of Polymer Based Drug Delivery Systems with Janus-Faced Function for Synergistic Targeted Drug Delivery and More Effective Cancer Therapy
Bacillus-Shape Design of Polymer Based Drug Delivery Systems with Janus-Faced Function for Synergistic Targeted Drug Delivery and More Effective Cancer Therapy
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具有两面功能的基于聚合物的药物递送系统的芽孢杆菌形状设计，用于协同靶向药物递送和更有效的癌症治疗。
DOI：
10.1021/mp500464b
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发表时间：
2015-04-01
影响因子：
4.9
通讯作者：
Hou, Zhenqing
中科院分区：
文献类型：
--
作者：
Cui, Fei;Lin, Jinyan;Hou, Zhenqing
药物递送系统的颗粒形状对其体外和体内性能有很大影响，但生产特定形状药物载体的技术有限。本文采用自组装技术制备了甲氨蝶呤（MTX）修饰的MPEG-PLA纳米芽孢杆菌（MPEG-PLA-MTX NB），并通过SPG膜在高N2压下挤出实现靶向给药。与MPEG-PLA-MTX纳米球（MPEG-PLA-MTX NS）和MPEG-PLA纳米球（MPEG-PLA NS）相比，MPEG-PLA-MTX NB表现出更高的体外和体内靶向效率。此外，MPEG-PLA-MTX纳米粒的体内外抗肿瘤活性也明显优于MPEG-PLA-MTX纳米粒和游离MTX注射液。据我们所知，这项工作提供了第一个例子的形状设计（介导的早期阶段的肿瘤积累和晚期细胞内化）和两面神面临的功能（介导的早期阶段的主动靶向作用和晚期抗癌作用）的基础上纳米级药物输送系统的整合。这种高度聚合和协同的给药策略为更多具有新形状和功能的药物递送系统的癌症治疗打开了大门。
The particle shape of the drug delivery systems had a strong impact on their in vitro and in vivo performance, but there was limited availability of techniques to produce the specific shaped drug carriers. In this article, the novel methotrexate (MTX) decorated MPEG-PLA nanobacillus (MPEG-PLA-MTX NB) was prepared by the self-assembly technique followed by the extrusion through SPG membrane with high N2 pressure for targeted drug delivery, in which Janus-like MTX was not only used as a specific anticancer drug but could also be served as a tumor-targeting ligand. The MPEG-PLA-MTX NBs demonstrated much higher in vitro and in vivo targeting efficiency compared to the MPEG-PLA-MTX nanospheres (MPEG-PLA-MTX NSs) and MPEG-PLA nanospheres (MPEG-PLA NSs). In addition, the MPEG-PLA-MTX NBs also displayed much more excellent in vitro and in vivo antitumor activity than the MPEG-PLA-MTX NSs and free MTX injection. To our knowledge, this work provided the first example of the integration of the shape design (which mediated an early phase tumor accumulation and a late-phase cell internalization) and Janus-faced function (which mediated an early phase active targeting effect and a late-phase anticancer effect) on the basis of nanoscaled drug delivery systems. The highly convergent and cooperative drug delivery strategy opens the door to more drug delivery systems with new shapes and functions for cancer therapy.