Low tumor specificity and multidrug resistance (MDR) remain challenging for many anticancer drugs. In this study, the micelles assembled by a matrix metalloproteinase 2 (MMP2)-sensitive self-assembling efflux inhibitor (PEG2k-pp-PE) were developed and evaluated in various cancer models. In vitro, the PEG2k-pp-PE micelles enhanced the cellular uptake and tissue penetration and sensitized the cancers to drug treatments in MDR cancer cells and their three-dimensional multicellular spheroids. Their efflux inhibitory capability was comparable to those of the well-known small-molecule P-glycoprotein (P-gp) inhibitor and polymeric P-gp inhibitor. In vivo, the PEG2k-pp-PE micelles could specifically and effectively deliver the loaded cargoes to the tumor, as evidenced by the enhanced drug accumulation and prolonged drug retention in the tumor tissue, resulting in the improved anticancer activity. Our results suggest that the PEG2k-pp-PE micelles may have great potential to be a simple but multifunctional nanocarrier for concurrent tumor-targeted drug delivery and sensitization of resistant cancers.

Qing Yao

Yin Liu

Longfa Kou

Ying Tu

Xing Tang

Lin Zhu

Nanomedicine Nanotechnology Biology and Medicine

NANOMEDICINE: NANOTECHNOLOGY, BIOLOGY, AND MEDICINE (NANOMEDICINE: NBM) 的使命是促进新兴的纳米医学跨学科领域。NANOMEDICINE: NBM 是一份国际性的、同行评审的期刊，展示与纳米医学相关的新颖、重要和跨学科的理论和实验结果生命和健康科学中的纳米科学和纳米技术。内容包括基础、转化和临床研究，涉及疾病的诊断、治疗、监测、预测和预防。

The mission of "Nanomedicine: Nanotechnology, Biology, and Medicine" is to advance the emerging interdisciplinary field of nanomedicine. This international, peer-reviewed journal showcases novel, significant, and interdisciplinary theoretical and experimental findings related to nanomedicine in the life and health sciences. The content includes basic, translational, and clinical research, addressing the diagnosis, treatment, monitoring, prediction, and prevention of diseases.

《Nanomedicine: Nanotechnology, Biology, and Medicine》（纳米医学：纳米技术、生物学与医学）的使命是推动新兴的纳米医学跨学科领域的发展。该期刊是一本国际性的、经过同行评审的期刊，展示与纳米医学相关的新颖、重要和跨学科的理论与实验成果，涵盖生命科学和健康科学中的纳米科学与纳米技术。内容包括基础研究、转化研究和临床研究，涉及疾病的诊断、治疗、监测、预测和预防。

Nanomedicine: Nanotechnology, Biology, and Medicine

Tumor-targeted drug delivery and sensitization by MMP2-responsive polymeric micelles

The results suggest that the PEG2k-pp-PE micelles may have great potential to be a simple but multifunctional nanocarrier for concurrent tumor-targeted drug delivery and sensitization of resistant cancers.

Category	Quartile
医学	2
医学, 医学研究与实验	3
医学, 纳米科技	3

Tumor-targeted drug delivery and sensitization by MMP2-responsive polymeric micelles

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Journal Info

Category	Quartile
NANOSCIENCE & NANOTECHNOLOGY	2