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Updated: May 16, 2025
Nanosensors to Detect Protease Activity In Vivo for Noninvasive Diagnostics
Published on: July 16, 2018
Self-Reporting Ratiometric AIEgen-Peptide Nanoprobes for Activatable Chemotherapy and Noninvasive Imaging of
Shicheng Pei1, Zhaohan Liu1, Qishu Jiao1
1Department of Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Abstract:
Efficacious chemotherapy and real-time therapeutic monitoring remain major challenges in cancer treatment. Traditional systems often lack tumor specificity, limiting efficacy, and hindering therapy optimization. Moreover, the absence of real-time monitoring can lead to missed opportunities and increased risks of side effects. Herein, we designed a self-reporting ratiometric AIEgen-peptide nanoprobe (TPE-1(Hyd-DOX)-DEVD) for activatable chemotherapy and noninvasive imaging of therapeutic outcomes. When doxorubicin (DOX) in the nanoprobe is selectively activated in the acidic tumor microenvironment, the ensuing caspase-3 cascade triggers a morphological transformation of the nanoprobe that amplifies the TPE fluorescence. This enhancement allows the TPE/DOX fluorescence ratio to serve as an indicator for monitoring DOX activation and for providing therapeutic feedback. Both in vitro and in vivo studies demonstrated that TPE-1(Hyd-DOX)-DEVD exhibited an impressive tumor suppression efficacy and excellent biocompatibility. This study highlights the strong potential of this nanoprobe as a valuable tool for cancer theranostics, offering hope for more effective and personalized treatment strategies.
Insights
This study introduces a novel nanoprobe for targeted cancer chemotherapy and real-time monitoring. The innovative design enables activatable drug release and visual feedback, improving treatment efficacy and safety.
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Chemotherapy efficacy and real-time monitoring are critical challenges in cancer treatment.
- Current methods often lack tumor specificity and real-time feedback, leading to suboptimal outcomes and potential side effects.
- There is a need for advanced theranostic tools for personalized cancer therapy.
Purpose of the Study:
- To design and evaluate a self-reporting ratiometric AIEgen-peptide nanoprobe for activatable chemotherapy and noninvasive imaging.
- To utilize the nanoprobe for real-time monitoring of drug activation and therapeutic outcomes.
- To assess the tumor suppression efficacy and biocompatibility of the developed nanoprobe.
Main Methods:
- Development of a ratiometric Aggregation-Induced Emission (AIE) gen-peptide nanoprobe (TPE-1(Hyd-DOX)-DEVD) incorporating doxorubicin (DOX).
- Investigation of selective DOX activation in the acidic tumor microenvironment and subsequent caspase-3 cascade triggering.
- Evaluation of nanoprobe morphological transformation and fluorescence amplification for therapeutic feedback.
- In vitro and in vivo studies to assess tumor suppression and biocompatibility.
Main Results:
- The nanoprobe demonstrated selective doxorubicin release and activation in the tumor microenvironment.
- Caspase-3 activation led to a morphological transformation, amplifying TPE fluorescence.
- The TPE/DOX fluorescence ratio effectively monitored DOX activation and provided therapeutic feedback.
- Significant tumor suppression efficacy and excellent biocompatibility were observed in both in vitro and in vivo models.
Conclusions:
- The developed nanoprobe serves as a powerful tool for activatable chemotherapy and real-time theranostic monitoring.
- This theranostic approach offers potential for more effective and personalized cancer treatment strategies.
- The nanoprobe shows promise for advancing cancer theranostics and improving patient outcomes.
