核黄素靶向聚合物可提高紫杉醇的耐受性,同时保持疗效。

IF 4.2 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Milita Darguzyte PhD , Elena Rama MSc , Anne Rix MSc , Jasmin Baier MSc , Juliane Hermann PhD , Sima Rezvantalab PhD , Mohammad Khedri MSc , Joachim Jankowski PhD , Fabian Kiessling MD
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引用次数: 0

摘要

主动靶向可以提高给药系统(DDS)治疗癌症的精确性和疗效。核黄素(RF)具有生物相容性,而且在癌症中的核黄素受体表达量很高,因此是一种很有前景的主动靶向配体。本研究评估了与紫杉醇(PTX)共轭的 RF 靶向 4 臂聚乙二醇(PEG)星,命名为 PEG PTX RF 靶向 DDS。在体外,与非靶向性对应物(PEG PTX)相比,PEG PTX RF 对肿瘤细胞的毒性更高,而游离 PTX 的急性毒性最高。在体内,所有治疗方法的效果相似,但经 PEG PTX RF 治疗的肿瘤细胞增殖较少,这表明治疗效果具有持续性。此外,PTX 治疗动物的体重和肝脏重量明显减轻,而 PEG PTX 和 PEG PTX RF 治疗动物的体重和肝脏重量均保持稳定。总之,我们的靶向和非靶向 DDS 减少了 PTX 的不良反应,射频靶向促进了癌细胞对药物的吸收,从而达到了持续治疗的效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Riboflavin-targeted polymers improve tolerance of paclitaxel while maintaining therapeutic efficacy

Riboflavin-targeted polymers improve tolerance of paclitaxel while maintaining therapeutic efficacy

Active targeting can enhance precision and efficacy of drug delivery systems (DDS) against cancers. Riboflavin (RF) is a promising ligand for active targeting due to its biocompatibility and high riboflavin-receptor expression in cancers. In this study, RF-targeted 4-arm polyethylene glycol (PEG) stars conjugated with Paclitaxel (PTX), named PEG PTX RF, were evaluated as a targeted DDS. In vitro, PEG PTX RF exhibited higher toxicity against tumor cells compared to the non-targeted counterpart (PEG PTX), while free PTX displayed the highest acute toxicity. In vivo, all treatments were similarly effective, but PEG PTX RF-treated tumors showed fewer proliferating cells, pointing to sustained therapy effects. Moreover, PTX-treated animals' body and liver weights were significantly reduced, whereas both remained stable in PEG PTX and PEG PTX RF-treated animals. Overall, our targeted and non-targeted DDS reduced PTX's adverse effects, with RF targeting promoted drug uptake in cancer cells for sustained therapeutic effect.

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来源期刊
CiteScore
11.10
自引率
0.00%
发文量
133
审稿时长
42 days
期刊介绍: The mission of Nanomedicine: Nanotechnology, Biology, and Medicine (Nanomedicine: NBM) is to promote the emerging interdisciplinary field of nanomedicine. Nanomedicine: NBM is an international, peer-reviewed journal presenting novel, significant, and interdisciplinary theoretical and experimental results related to nanoscience and nanotechnology in the life and health sciences. Content includes basic, translational, and clinical research addressing diagnosis, treatment, monitoring, prediction, and prevention of diseases.
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