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Design of prodrugs with reactive oxygen species as activators and their application in tumor therapy
Jiaqi Xing1, Wenjuan Lu1, Yubing Zhang1
1State Key Laboratory of Advanced Drug Delivery and Release Systems, Key Laboratory for Biotechnology Drugs of National Health Commission, Key Laboratory of Rare and Rare Diseases in Shandong Province, School of Pharmacy (Institute of Pharmacy) of Shandong First Medical University, Jinan, Shandong 250117, China.
Abstract:
Major challenges lie in the precise management (encompassing diagnosis and treatment) of malignant neoplasms. Traditional chemotherapy faces restrictions in clinical use because of its ineffective targeting and significant toxicity, along with side effects. Notably, the ROS levels are observably elevated in cancer cells compared to healthy tissues, which presents a distinct opportunity for the creation of prodrugs that respond to ROS. This article systematically reviewed the research progress on ROS-responsive small molecule prodrugs and nanodelivery systems (including polymer/inorganic nanoparticles and hydrogels) over the past five years and elaborated in detail on the design principles based on seven key activation mechanisms. By combining ROS responsiveness with TME specificity, these systems have achieved precise controlled drug release, significantly reduced toxic and side effects, and demonstrated multiple synergistic effects of chemotherapy, immunotherapy, and photodynamic therapy. Additionally, some systems integrate theranostic and imaging functions, allowing real-time observation of the drug release. Subsequently, the latest progress in the field from molecular design to preclinical research was summarized, and the promise of ROS-responsive systems for clinical applications was emphasized. It directs the creation of prodrugs that are highly specific and supports the advancement of multi-responsive theranostic platforms, thereby paving the way for improved precision in the diagnosis and treatment of tumors.
Insights
Reactive oxygen species (ROS)-responsive prodrugs and nanodelivery systems offer precise cancer treatment by targeting elevated ROS levels in tumors. These advanced systems enhance drug delivery, reduce side effects, and enable combination therapies for improved tumor management.
Area of Science:
- Oncology
- Materials Science
- Drug Delivery
Background:
- Malignant neoplasms present significant diagnostic and treatment challenges.
- Traditional chemotherapy has limitations due to poor targeting, toxicity, and side effects.
- Elevated reactive oxygen species (ROS) in cancer cells offer a target for novel prodrug strategies.
Purpose of the Study:
- To systematically review research on ROS-responsive small molecule prodrugs and nanodelivery systems.
- To elaborate on design principles based on key activation mechanisms.
- To summarize recent advancements and future potential for clinical applications.
Main Methods:
- Systematic literature review of ROS-responsive prodrugs and nanodelivery systems (nanoparticles, hydrogels) from the past five years.
- Analysis of seven key activation mechanisms for ROS responsiveness.
- Evaluation of combined ROS responsiveness with tumor microenvironment (TME) specificity.
Main Results:
- ROS-responsive systems achieve precise, controlled drug release.
- These systems significantly reduce toxic and side effects compared to traditional chemotherapy.
- Demonstrated synergistic effects through combination therapy (chemotherapy, immunotherapy, photodynamic therapy).
- Integrated theranostic and imaging functions allow real-time drug release monitoring.
Conclusions:
- ROS-responsive prodrugs and nanodelivery systems show great promise for precise tumor diagnosis and treatment.
- These platforms enhance specificity, reduce toxicity, and enable multi-modal therapeutic strategies.
- Further development is crucial for advancing these systems towards clinical application.
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