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Purpose <p>One of the hallmarks of cancer cells is their elevated levels of reactive oxygen species (ROS) compared with normal cells. Capitalizing on this, a novel paclitaxel (PTX, a first-line chemotherapeutic agent) prodrug was designed and synthesized by attaching a cinnamaldehyde (CA) molecule to PTX via a ROS-responsive thioacetal group.</p> Methods <p>The paclitaxel prodrug (PTX-S-CA) prodrug was synthesized and characterized, followed by self-assembly into nanoparticles (NPs) using DSPE-PEG<sub>2K</sub> as a stabilizer, forming PTX-S-CA/DSPE-PEG<sub>2K</sub> NPs. The physicochemical properties of the NPs were evaluated, which included drug-loading capacity, encapsulation efficiency, and plasma stability. In vitro cytotoxicity assays were conducted on cancer cells, and in vivo anti-tumor efficacy was assessed in a murine tumor model. The pharmacokinetics of the NPs were also studied in rats.</p> Results <p>In the tumor microenvironment, the ROS-sensitive thioacetal group in PTX-S-CA was degraded due to high ROS levels, leading to the release of both PTX and CA. The released CA synergistically enhanced the anti-tumor effects of PTX by inducing additional ROS production within the mitochondria. The NPs demonstrated a high loading capacity and encapsulation efficiency for PTX-S-CA, high cytotoxicity against cancer cells, excellent anti-tumor effects on mice, and high plasma stability in rats.</p> Conclusion <p>The use of the NP drug delivery platform served as a potentially effective therapeutic strategy for treating tumors, especially breast cancer.</p>

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ROS-activated prodrug nano-assemblies based on cinnamaldehyde-modified paclitaxel for treating breast cancer

  • 期刊论文

  • 发表日期：

    2025年5月27日

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  • Yali Chen,
  • Lei Qian,
  • Chunyun Xu,
  • Hongjie Huo,
  • Zhenya Sun,
  • Hongyang Zhang,
  • Shuang Yuan,
  • Yan Qi,
  • Peng Chu,
  • Lixue Chen,
  • Yanfang Ding,
  • Lei Li

摘要

Purpose

One of the hallmarks of cancer cells is their elevated levels of reactive oxygen species (ROS) compared with normal cells. Capitalizing on this, a novel paclitaxel (PTX, a first-line chemotherapeutic agent) prodrug was designed and synthesized by attaching a cinnamaldehyde (CA) molecule to PTX via a ROS-responsive thioacetal group.

Methods

The paclitaxel prodrug (PTX-S-CA) prodrug was synthesized and characterized, followed by self-assembly into nanoparticles (NPs) using DSPE-PEG2K as a stabilizer, forming PTX-S-CA/DSPE-PEG2K NPs. The physicochemical properties of the NPs were evaluated, which included drug-loading capacity, encapsulation efficiency, and plasma stability. In vitro cytotoxicity assays were conducted on cancer cells, and in vivo anti-tumor efficacy was assessed in a murine tumor model. The pharmacokinetics of the NPs were also studied in rats.

Results

In the tumor microenvironment, the ROS-sensitive thioacetal group in PTX-S-CA was degraded due to high ROS levels, leading to the release of both PTX and CA. The released CA synergistically enhanced the anti-tumor effects of PTX by inducing additional ROS production within the mitochondria. The NPs demonstrated a high loading capacity and encapsulation efficiency for PTX-S-CA, high cytotoxicity against cancer cells, excellent anti-tumor effects on mice, and high plasma stability in rats.

Conclusion

The use of the NP drug delivery platform served as a potentially effective therapeutic strategy for treating tumors, especially breast cancer.