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Updated: Jan 2, 2026
Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
pH-Driven Targeting Nanoprobe with Dual-Responsive Drug Release for Persistent Luminescence Imaging and Chemotherapy
Hong-Jiao Zhang1, Xu Zhao2,3,4, Li-Jian Chen2,3,4
1Research Center for Analytical Sciences, Tianjin Key Laboratory of Molecular Recognition and Biosensing , College of Chemistry, Nankai University , Tianjin , 300071 , China.
Abstract:
Multifunctional nanoprobes with both imaging and drug delivery capabilities represent an emerging approach to the diagnosis and treatment of tumor. However, poor accumulation in tumor cells and low drug availability are the main limitations for their further application. Here we show a pH-driven targeting nanoprobe with dual-responsive drug release for persistent luminescence imaging and chemotherapy of tumor. The nanoprobe is constructed by conjugating the pH-low-insertion-peptide (pHLIP) to the surface of the core-shell structure of mesoporous silica-coated persistent luminescence nanoparticles (MSPLNPs) with the peptide GFLG and disulfide bond as bridges. The pHLIP functionalized nanoprobe exhibits higher cellular uptake for A549 and HepG2 cells in an acidic extracellular microenvironment (pH < 6.5) than in normal physiological condition (pH 7.4). The nanoprobe possesses well-defined NIR persistent luminescence performance and can be effectively accumulated in the tumor site, leading to the visual HepG2 tumor target imaging without autofluorescence interference. Furthermore, the nanoprobe realizes the dual-responsive release of doxorubicin loaded in the mesoporous channels in systems containing cathepsin B and glutathione, and can effectively kill tumor cells and inhibit the growth of tumor. This integrated nanoprobe possesses great potential for the diagnosis and treatment of tumors with high specificity and efficiency.
Insights
This study introduces a pH-responsive nanoprobe for targeted tumor imaging and chemotherapy. The novel design enhances drug delivery and tumor cell uptake, improving treatment efficacy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Multifunctional nanoprobes offer combined imaging and drug delivery for cancer diagnosis and treatment.
- Key limitations include poor tumor cell accumulation and low drug availability.
Purpose of the Study:
- To develop a pH-driven targeting nanoprobe with dual-responsive drug release for persistent luminescence imaging and chemotherapy.
- To overcome limitations of current nanoprobes for enhanced tumor targeting and treatment efficiency.
Main Methods:
- Constructed a nanoprobe by conjugating pH-low-insertion-peptide (pHLIP) to mesoporous silica-coated persistent luminescence nanoparticles (MSPLNPs).
- Utilized peptide GFLG and disulfide bonds as bridges for functionalization.
- Loaded doxorubicin into mesoporous channels for drug delivery.
Main Results:
- pHLIP functionalization increased cellular uptake in acidic tumor microenvironments (pH < 6.5).
- The nanoprobe demonstrated effective near-infrared persistent luminescence for visual tumor imaging.
- Dual-responsive drug release (cathepsin B and glutathione) led to effective tumor cell killing and growth inhibition.
Conclusions:
- The integrated nanoprobe shows high specificity and efficiency for tumor diagnosis and treatment.
- This approach holds significant potential for advancing cancer therapy and imaging.
