A Comparative Evaluation of Hydroxycamptothecin Drug Nanorods With and Without Methotrexate Prodrug Functionalization for Drug Delivery.

A Comparative Evaluation of Hydroxycamptothecin Drug Nanorods With and Without Methotrexate Prodrug Functionalization for Drug Delivery.
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具有和不具有甲氨蝶呤前药功能化的羟基喜树碱药物纳米棒用于药物递送的比较评价

DOI:
10.1186/s11671-016-1599-y
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发表时间:
2016-12
影响因子:
--
通讯作者:
Hou Z
Hou Z
中科院分区:
材料科学3区
文献类型:
--
作者:
Guo F;Fan Z;Yang J;Li Y;Wang Y;Zhao H;Xie L;Hou Z

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我们开发了一种新型的自靶向多药共递送系统,该系统基于棒状10-羟基喜树碱(CPT)纳米抗癌药物(CPT NRs),然后用自靶向聚乙二醇化脂质缀合的甲氨蝶呤(MTX)前体抗癌药物进行表面功能化。通过比较PEG-CPT NR的细胞摄取和MTT测定,证明了MTX-PEG-CPT NR对HeLa细胞的自靶向作用和体外细胞活力。体外研究表明,使用这种高载药量MTX-PEG-CPT NR在自靶向给药、控释/缓释和协同癌症治疗中的可行性。更重要的是,这项工作将通过引入早期肿瘤靶向作用,然后驱动晚期抗癌作用来刺激对使用PEG化脂质缀合的MTX的兴趣,用于纳米多药物的高度收敛设计,这可能有利地提供了一种新的简单策略,用于同时靶向和治疗FA受体过表达的癌细胞。本文的在线版本(doi:10.1186/s11671-016-1599-y)包含补充材料,可供授权用户使用。
We developed a novel self-targeted multi-drug co-delivery system based on rod-shaped 10-hydroxycamptothecin (CPT) nanoanticancer drug (CPT NRs) followed by a surface functionalization with self-targeting PEGylated lipid-conjugated methotrexate (MTX) pro-anticancer drug. The self-targeting effect and in vitro cell viability of the MTX-PEG-CPT NRs on HeLa cells were demonstrated by comparative cellular uptake and MTT assay of the PEG-CPT NRs. In vitro studies showed the feasibility of using this high drug-loading MTX-PEG-CPT NRs in self-targeted drug delivery, controlled-/sustained-release, and synergistic cancer therapy. More importantly, this work would stimulate interest in the use of PEGylated lipid-conjugated MTX by introducing an early-phase tumor-targeting role and then driving a late-phase anticancer role for the highly convergent design of nanomulti-drug, which may advantageously offer a new and simple strategy for simultaneously targeting and treating FA receptor-overexpressing cancer cells. The online version of this article (doi:10.1186/s11671-016-1599-y) contains supplementary material, which is available to authorized users.
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