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Hypoxia-Responsive Thio-Perylene Diimides Delivered via pH-Responsive Polypeptide Nanoparticles: Toward a Combination
Yushen Kang1, He Ma1, Huacheng Yu1
1Key Lab of Organic Optoelectronics & Molecular Engineering, Department of Chemistry, Tsinghua University, Beijing 100084, China.
Abstract:
Developing responsive therapeutic systems based on the tumor microenvironment is crucial for efficient and specific treatments. However, how to achieve sensitive response and efficient anticancer bioactivity remains a challenge. Here, tumor-responsive polypeptide nanoparticles encapsulating thio-perylene diimides are constructed. Anticancer peptides were released through the hydrolysis of acid-labile amide bonds to induce cell apoptosis, while thio-perylene diimide radical anions with up to 67% NIR photothermal conversion efficiency could be generated through a hypoxia-induced biological reduction process. Thus, this approach enables the development of a dual-response nanomedicine to achieve combinational NIR photothermal therapy and chemotherapy. In the A549 lung cancer cell-derived xenograft model established in BALB/c nude mice, the tumor inhibition rate reached 68.0%. In addition, tumor-responsive polypeptide nanoparticles also possessed excellent biocompatibility. This line of research provides a new method for the construction of highly sensitive tumor microenvironment-responsive therapeutic systems and contributes to the development of comprehensive multimodal treatment approaches.
Insights
This study developed dual-responsive nanoparticles that combine chemotherapy and photothermal therapy for cancer treatment. The novel nanomedicine demonstrated significant tumor inhibition and excellent biocompatibility in preclinical models.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Therapy
Background:
- Developing tumor microenvironment-responsive therapeutic systems is essential for targeted cancer treatment.
- Achieving both sensitive response and potent anticancer activity in nanomedicines remains a significant challenge.
Purpose of the Study:
- To construct tumor-responsive polypeptide nanoparticles encapsulating thio-perylene diimides for combined photothermal and chemotherapy.
- To investigate the dual-response mechanism and evaluate the therapeutic efficacy and biocompatibility of the developed nanomedicine.
Main Methods:
- Synthesis of polypeptide nanoparticles encapsulating thio-perylene diimides.
- Utilizing acid-labile amide bond hydrolysis for anticancer peptide release and hypoxia-induced reduction for NIR photothermal conversion.
- Evaluating therapeutic efficacy in an A549 lung cancer xenograft mouse model.
Main Results:
- The nanoparticles demonstrated dual-responsive drug release and efficient near-infrared (NIR) photothermal conversion (up to 67%).
- A significant tumor inhibition rate of 68.0% was achieved in the A549 lung cancer xenograft model.
- The developed nanomedicine exhibited excellent biocompatibility.
Conclusions:
- This approach provides a novel method for constructing highly sensitive tumor microenvironment-responsive therapeutic systems.
- The dual-responsive nanomedicine offers a promising strategy for combinational photothermal therapy and chemotherapy.
- This research contributes to the development of advanced multimodal cancer treatment strategies.
