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Aggregation-Caused Quenching Dyes as Potent Tools to Track the Integrity of Antitumor Nanocarriers: A Mini-Review
Xiye Wang1, Jiayue Huang1, Mengqin Guo1
1State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510006, China.
Abstract:
Cancer has become one of the major causes of death worldwide. Chemotherapy remains a cornerstone of cancer treatment. To enhance the tumor-targeting efficiency of chemotherapy agents, pharmaceutical scientists have developed nanocarriers. However, the in vivo structural integrity and dynamic changes in nanocarriers after administration are not well understood, which may significantly impact their tumor-targeting abilities. In this paper, we propose the use of environmentally responsive fluorescent probes to track the integrity of antitumor nanocarriers. We compare three main types of dyes: fluorescence resonance energy transfer (FRET) dyes, aggregation-induced emission (AIE) dyes, and aggregation-caused quenching (ACQ) dyes. Among them, ACQ dyes, possessing sensitive water-quenching properties and easily detected "on-off" switching behavior, are regarded as the most promising choice. We believe that ACQ dyes are suitable for investigating the in vivo fate of antitumor nanocarriers and can aid in designing improved nanoformulations for chemotherapy agents.
Insights
Aggregation-caused quenching (ACQ) dyes effectively track antitumor nanocarrier integrity in vivo. These environmentally responsive fluorescent probes offer promising insights for improving chemotherapy nanoformulations and tumor targeting.
Area of Science:
- Pharmaceutical Sciences
- Biomedical Engineering
- Materials Science
Background:
- Cancer remains a leading global cause of mortality, with chemotherapy as a primary treatment modality.
- Nanocarriers enhance tumor-targeting efficiency of chemotherapy agents, but their in vivo behavior is poorly understood.
- Understanding nanocarrier structural integrity and dynamic changes is crucial for optimizing drug delivery.
Purpose of the Study:
- To investigate the use of environmentally responsive fluorescent probes for tracking antitumor nanocarrier integrity in vivo.
- To compare the efficacy of fluorescence resonance energy transfer (FRET), aggregation-induced emission (AIE), and aggregation-caused quenching (ACQ) dyes for this purpose.
- To identify the most suitable dye type for monitoring nanocarrier fate and informing future nanoformulation design.
Main Methods:
- Evaluation of three distinct classes of fluorescent dyes: FRET, AIE, and ACQ dyes.
- Assessment of dye responsiveness to environmental changes relevant to in vivo conditions.
- Comparative analysis of dye performance in tracking nanocarrier structural integrity.
Main Results:
- Aggregation-caused quenching (ACQ) dyes exhibit sensitive water-quenching properties.
- ACQ dyes demonstrate easily detectable "on-off" switching behavior, indicative of structural changes.
- These characteristics make ACQ dyes highly suitable for monitoring nanocarrier integrity.
Conclusions:
- Aggregation-caused quenching (ACQ) dyes are the most promising fluorescent probes for tracking antitumor nanocarrier integrity in vivo.
- ACQ dyes facilitate the investigation of nanocarrier fate and structural dynamics after administration.
- This approach can significantly aid in the design of improved nanoformulations for enhanced chemotherapy efficacy.

