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ROS-Responsive Micelles Loaded with Podophyllotoxin Inhibit Tumor Growth via ROS Self-Amplification and Regulation of
Shuaiheng Song1, Qiang Shao1, Siyi Liang1
1Department of Organic Chemistry, College of Pharmacy, Harbin Medical University, Harbin 150081, China.
International Journal of Molecular Sciences
|August 13, 2026
Summary
This study developed a novel micelle system that releases podophyllotoxin (PPT) in response to reactive oxygen species (ROS) found in tumors. This targeted delivery enhances anticancer efficacy and reduces side effects for lung and breast cancer treatment.
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Podophyllotoxin (PPT) exhibits anticancer properties against lung and breast cancers but suffers from poor solubility and severe side effects, limiting its clinical use.
- Tumor microenvironments have higher reactive oxygen species (ROS) levels than normal tissues, presenting an opportunity for targeted drug delivery.
- Developing stimuli-responsive drug delivery systems is crucial for improving chemotherapeutic efficacy and patient safety.
Purpose of the Study:
- To design and fabricate a ROS-responsive micelle delivery system for podophyllotoxin (PPT).
- To evaluate the PPT release kinetics, drug loading, and stability of the developed micelles.
- To assess the in vitro and in vivo antitumor efficacy and biosafety of the ROS-responsive PPT-loaded micelles (M@PPT).
Main Methods:
- Fabrication of blank (M) and PPT-loaded (M@PPT) micelles.
- Characterization of micelle particle size, uniformity, colloidal stability, and biosafety.
- Assessment of ROS-responsive drug release using HPLC and DCFH-DA assays.
- In vitro cellular assays evaluating apoptosis, cell cycle arrest, and protein expression.
- In vivo studies to confirm antitumor efficacy and biosafety.
Main Results:
- Micelles (M and M@PPT) demonstrated good particle size uniformity, stability, and biosafety.
- Blank micelles showed ROS-responsive swelling and drug release upon H2O2 exposure, confirming the system's responsiveness.
- M@PPT achieved significant PPT release in the presence of ROS, creating a positive feedback loop that enhanced drug release.
- M@PPT exhibited superior in vitro tumor growth inhibition compared to free PPT via apoptosis induction and cell cycle arrest.
- In vivo studies confirmed enhanced antitumor efficacy and improved biosafety of M@PPT over free PPT.
Conclusions:
- The developed ROS-responsive micellar system effectively delivers PPT in a targeted manner.
- This system enhances PPT's antitumor activity by leveraging the tumor microenvironment's ROS levels.
- The ROS-responsive micelles offer a promising strategy to overcome PPT's limitations and improve its clinical application in cancer therapy.
