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Updated: Jun 14, 2026
Computed Tomography-guided Time-domain Diffuse Fluorescence Tomography in Small Animals for Localization of Cancer Biomarkers
Published on: July 17, 2012
Cancer Cell-Specific Fluorescent Prodrug Delivery Platforms
Siyue Ma1,2, Ji Hyeon Kim3, Wei Chen4
1The Youth Innovation Team of Shaanxi Universities, Shaanxi Key Laboratory of Chemical Additives for Industry, College of Chemistry and Chemical Engineering, Shaanxi University of Science & Technology, Xi'an, 710021, China.
Abstract:
Targeting cancer cells with high specificity is one of the most essential yet challenging goals of tumor therapy. Because different surface receptors, transporters, and integrins are overexpressed specifically on tumor cells, using these tumor cell-specific properties to improve drug targeting efficacy holds particular promise. Targeted fluorescent prodrugs not only improve intracellular accumulation and bioavailability but also report their own localization and activation through real-time changes in fluorescence. In this review, efforts are highlighted to develop innovative targeted fluorescent prodrugs that efficiently accumulate in tumor cells in different organs, including lung cancer, liver cancer, cervical cancer, breast cancer, glioma, and colorectal cancer. The latest progress and advances in chemical design and synthetic considerations in fluorescence prodrug conjugates and how their therapeutic efficacy and fluorescence can be activated by tumor-specific stimuli are reviewed. Additionally, novel perspectives are provided on strategies behind engineered nanoparticle platforms self-assembled from targeted fluorescence prodrugs, and how fluorescence readouts can be used to monitor the position and action of the nanoparticle-mediated delivery of therapeutic agents in preclinical models. Finally, future opportunities for fluorescent prodrug-based strategies and solutions to the challenges of accelerating clinical translation for the treatment of organ-specific tumors are proposed.
Insights
Targeted fluorescent prodrugs offer precise cancer therapy by accumulating in tumor cells and signaling their location. This review explores advances in their design and application for various organ-specific cancers.
Area of Science:
- Oncology
- Biomedical Engineering
- Medicinal Chemistry
Background:
- Achieving high specificity in tumor therapy remains a significant challenge.
- Tumor cells overexpress specific surface receptors, transporters, and integrins, presenting opportunities for targeted drug delivery.
- Targeted fluorescent prodrugs enhance drug accumulation and bioavailability while providing real-time localization and activation feedback.
Purpose of the Study:
- To review the development of innovative targeted fluorescent prodrugs for efficient tumor cell accumulation.
- To highlight chemical design and synthetic strategies for fluorescence prodrug conjugates.
- To explore nanoparticle platforms for targeted drug delivery and fluorescence monitoring in preclinical models.
Main Methods:
- Review of literature on targeted fluorescent prodrugs for various cancers (lung, liver, cervical, breast, glioma, colorectal).
- Analysis of chemical design, synthesis, and activation mechanisms of fluorescence prodrug conjugates.
- Examination of engineered nanoparticle platforms utilizing targeted fluorescent prodrugs.
Main Results:
- Targeted fluorescent prodrugs demonstrate efficient accumulation in tumor cells across different organs.
- Therapeutic efficacy and fluorescence activation are linked to tumor-specific stimuli.
- Fluorescence readouts enable monitoring of nanoparticle-mediated drug delivery in preclinical studies.
Conclusions:
- Targeted fluorescent prodrugs represent a promising strategy for organ-specific cancer treatment.
- Advances in chemical design and nanoparticle engineering are crucial for therapeutic efficacy.
- Addressing challenges in clinical translation is key to accelerating the adoption of these strategies.
