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首页> 外文期刊>Advanced Functional Materials >Platinum on Nanodiamond: A Promising Prodrug Conjugated with Stealth Polyglycerol, Targeting Peptide and Acid-Responsive Antitumor Drug
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Platinum on Nanodiamond: A Promising Prodrug Conjugated with Stealth Polyglycerol, Targeting Peptide and Acid-Responsive Antitumor Drug

机译：纳米金刚石上的铂：一种有前途的前药，与隐形聚甘油，靶向肽和酸响应性抗肿瘤药结合在一起

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摘要

In the field of nanomedicine, nanoparticles with various functions are required for in vivo applications such as biomedical imaging and drug delivery. Therefore, chemical functionalization of nanoparticles has been extensively investigated. Herein, nanodiamond (ND) coated with polyglycerol (PG) and its derivatives is reported to impart good solubility in a physiological environment, a stealth nature to avoid nonspecific uptake, a targeting property to be taken up by a specific cell, and an acid-responsive drug release property to kill cancer cells. ND is first grafted with PG and the resulting ND-PC has a high solubility in physiological media. Since a large number of hydroxyl groups in PC provide scaffolds for further surface functionalization, the targeting RGD peptide and Pt-based drug are immobilized to give ND-PG-RgD, ND-PG-Pt and ND-PG-RGD-Pt. The ND with intrinsic fluorescence is also functionalized by PC and RGD to confirm cellular uptake and intracellular localization fluo-rescently. The results of the cell experiments indicate that PC coating shielded fND from the uptake by HeLa and U87MG cells. In contrast, fMD-PG-RGD is taken up by U87MG, not HeLa cells, exhibiting high targeting efficacy. When ND-PG-RGD-Pt is applied, U87MG is selectively killed against HeLa. The multi-functional ND is a promising prodrug in targeting chemotherapy.
机译：在纳米医学领域，体内应用例如生物医学成像和药物递送需要具有各种功能的纳米颗粒。因此，已经广泛研究了纳米颗粒的化学功能化。在此，据报道，涂有聚甘油（PG）及其衍生物的纳米金刚石（ND）在生理环境中具有良好的溶解性，可避免非特异性吸收的隐形特性，可被特定细胞吸收的靶向特性以及酸-响应性药物释放特性可杀死癌细胞。首先用PG接枝ND，所得的ND-PC在生理介质中具有高溶解度。由于PC中的大量羟基为进一步的表面功能化提供了支架，因此将靶向RGD肽和Pt基药物固定化，得到ND-PG-RgD，ND-PG-Pt和ND-PG-RGD-Pt。具有内在荧光的ND也可以通过PC和RGD进行功能化，以确认细胞的摄取和荧光的细胞内定位。细胞实验结果表明，PC涂层可屏蔽fND使其免受HeLa和U87MG细胞的摄取。相比之下，fMD-PG-RGD由U87MG而非HeLa细胞吸收，表现出高靶向效果。当使用ND-PG-RGD-Pt时，U87MG被选择性杀灭HeLa。多功能ND是靶向化疗的有前途的前药。

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  • 来源
    《Advanced Functional Materials》 |2014年第34期|5348-5357|共10页
  • 作者

    Li Zhao; Yong-Hong Xu; Hongmei Qin; Shigeaki Abe; Tsukasa Akasaka; Tokuhiro Chano; Fumio Watari; Takahide Kimura; Naoki Komatsu; Xiao Chen;

  • 作者单位

    Department of Chemistry Shiga University of Medical Science, Seta Otsu 520-2192, Japan;

    Institute of Ophthalmological Research Department of Ophthalmology Renmin Hospital of Wuhan University Wuhan 430060, China;

    Department of Chemistry Shiga University of Medical Science, Seta Otsu 520-2192, Japan;

    Department of Biomedical Dental Materials and Engineering Graduate School of Dental Medicine Hokkaido University Sapporo 060-8586, Japan;

    Department of Biomedical Dental Materials and Engineering Graduate School of Dental Medicine Hokkaido University Sapporo 060-8586, Japan;

    Department of Clinical Laboratory Medicine Shiga University of Medical Science Seta, Otsu 520-2192, Japan;

    Department of Biomedical Dental Materials and Engineering Graduate School of Dental Medicine Hokkaido University Sapporo 060-8586, Japan;

    Department of Chemistry Shiga University of Medical Science, Seta Otsu 520-2192, Japan;

    Department of Chemistry Shiga University of Medical Science, Seta Otsu 520-2192, Japan;

    Department of Biomedical Dental Materials and Engineering Graduate School of Dental Medicine Hokkaido University Sapporo 060-8586, Japan;

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