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首页> 外文期刊>Molecular pharmaceutics >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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Bacillus-shape design of polymer based drug delivery systems with janus-faced function for synergistic targeted drug delivery and more effective cancer therapy.

机译：基于聚合物的药物传递系统的芽孢杆菌形状设计，具有双侧表面功能，可协同靶向药物传递和更有效的癌症治疗。

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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.
机译：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，但是生产特定形状的药物载体的技术有限。在本文中，通过自组装技术制备了新型甲氨蝶呤（MTX）装饰的MPEG-PLA纳米杆菌（MPEG-PLA-MTX NB），然后通过具有高N2压力的SPG膜挤出以靶向药物递送，样MTX不仅用作特定的抗癌药，而且还可以用作靶向肿瘤的配体。与MPEG-PLA-MTX纳米球（MPEG-PLA-MTX NSs）和MPEG-PLA纳米球（MPEG-PLA NSs）相比，MPEG-PLA-MTX NB在体内外的靶向效率更高。此外，MPEG-PLA-MTX NBs在体外和体内的抗肿瘤活性也比MPEG-PLA-MTX NS和自由MTX注射剂更好。据我们所知，这项工作提供了整合形状设计（介导早期肿瘤积累和晚期细胞内化）和Janus-faced功能（介导早期主动靶向作用和晚期阶段的抗癌作用）。高度融合和合作的药物输送策略为癌症治疗的新形状和功能的更多药物输送系统打开了大门。

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