Related Experiment Video
Updated: Jan 13, 2026
Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
Published on: February 17, 2023
Spatiotemporal control of prodrug activation through external stimuli for effective and safe on-site release in solid
Gabriele La Monica1, Alessia Bono2, Federica Alamia1
1Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche "STEBICEF", University of Palermo, Viale delle Scienze- Ed. 17, 90128 Palermo, Italy.
Abstract:
Achieving precise control over anticancer drug activity remains a key challenge in prodrug design. Stimuli-responsive systems address this limitation by enabling selective drug release within the tumor microenvironment. Among them, externally activated prodrugs (triggered by light, ionizing radiation, or ultrasound) offer superior spatial and temporal precision, with minimal systemic toxicity. This review critically examines recent advances in design strategies, activation mechanisms, and the translational potential of these systems, including both organic photocages and emerging metal-based platforms [e.g. Pt(IV) and Ru(II) complexes]. Particular attention is given to their integration with next-generation therapeutic modalities such as proteolysis-targeting chimeras (PROTACs) and antibody-drug conjugates (ADCs). Externally triggered prodrug technologies are poised to redefine precision oncology by improving efficacy, safety, and on-demand activation from molecular design to preclinical validation.
Insights
Externally activated prodrugs offer precise anticancer drug delivery, minimizing toxicity. This review explores advanced designs and activation methods for improved precision oncology applications.
Area of Science:
- Medicinal Chemistry
- Oncology
- Materials Science
Background:
- Controlling anticancer drug activity is crucial for effective prodrug design.
- Stimuli-responsive prodrugs enable targeted drug release in the tumor microenvironment.
- Externally activated prodrugs provide enhanced spatial and temporal control with reduced systemic toxicity.
Purpose of the Study:
- To review recent advancements in externally activated prodrug systems.
- To examine design strategies, activation mechanisms, and translational potential.
- To highlight integration with novel therapeutic modalities like PROTACs and ADCs.
Main Methods:
- Literature review of stimuli-responsive prodrugs.
- Analysis of organic photocages and metal-based platforms (e.g., Pt(IV), Ru(II)).
- Examination of prodrug integration with proteolysis-targeting chimeras (PROTACs) and antibody-drug conjugates (ADCs).
Main Results:
- Externally activated prodrugs demonstrate superior precision in drug release.
- Both organic and metal-based platforms show promise for targeted cancer therapy.
- Integration with PROTACs and ADCs expands therapeutic possibilities.
Conclusions:
- Externally triggered prodrugs are key to advancing precision oncology.
- These systems improve therapeutic efficacy and safety through on-demand activation.
- Significant potential exists from molecular design through preclinical validation.
More Related Videos
07:47Custom-designed Laser-based Heating Apparatus for Triggered Release of Cisplatin from Thermosensitive Liposomes with Magnetic Resonance Image Guidance
Published on: December 13, 2015
13:17In Vitro and In Vivo Evaluation of Photocontrolled Biologically Active Compounds - Potential Drug Candidates for Cancer Photopharmacology
Published on: September 29, 2023
