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Aptamer-Pyropheophorbide a Conjugates with Tumor Spheroid Targeting and Penetration Abilities for Photodynamic
Hongjie Xiong1, Jianhua Yan1, Shundong Cai1
1Department of Pharmaceutics, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, 410013 Hunan Province, P. R. China.
Abstract:
Pyropheophorbide a (Pyro) is a widely used photosensitizer for photodynamic therapy (PDT). However, poor water solubility, aggregation-induced fluorescence quenching, and lack of selectivity to targeted cells seriously limit its application. In this work, we prepared aptamer-Pyro conjugates (APCs) by linking Pyro to hydrophilic nucleic acid aptamer to enhance its water solubility and endow it with protein tyrosine kinase 7 (PTK7) overexpressed tumor spheroid specific targeting and penetration abilities for photodynamic therapy. The molecular conjugate was successfully synthesized and dissolved well in an aqueous solution. The APCs showed strong near-infrared fluorescence in the aqueous solution and produced singlet oxygen both in the solution and cells under laser irradiation, indicating its generation of singlet oxygen during PDT was guaranteed. Owing to the cancer cell targeting ability of the aptamer, the APCs specifically bound with PTK7 overexpressed cancerous cells and showed fluorescence signal for tumor cell imaging and diagnosis. The APCs exhibited favorable enhanced phototoxicity to target tumor cells compared with control cells. More importantly, due to the small size of the molecular conjugate, the APCs efficiently penetrated into the interior of multicellular tumor spheroids (MCTS) and caused cell damage. All these results indicated that the robust aptamer-Pyro conjugate is a promising selective tumor-targeting and penetrable molecule for cancer photodynamic therapy.
Insights
This study developed aptamer-pyropheophorbide a conjugates (APCs) for enhanced photodynamic therapy (PDT). These APCs improve water solubility, target cancer cells, and penetrate tumors, offering a promising solution for selective cancer treatment.
Area of Science:
- Biomedical Engineering
- Photodynamic Therapy
- Cancer Therapeutics
Background:
- Pyropheophorbide a (Pyro) is a photosensitizer used in photodynamic therapy (PDT), but its clinical application is limited by poor water solubility, aggregation-caused quenching, and lack of cell selectivity.
- Targeted delivery and improved physicochemical properties are crucial for enhancing the efficacy of photosensitizers in PDT.
Purpose of the Study:
- To develop aptamer-pyropheophorbide a conjugates (APCs) for improved water solubility, enhanced tumor targeting, and increased penetration for photodynamic therapy.
- To evaluate the efficacy of APCs in targeting protein tyrosine kinase 7 (PTK7) overexpressing cancer cells and their potential for tumor imaging and diagnosis.
Main Methods:
- Synthesis of aptamer-pyropheophorbide a conjugates (APCs) by linking Pyro to a hydrophilic nucleic acid aptamer.
- Characterization of APCs' water solubility, fluorescence properties, and singlet oxygen generation under laser irradiation.
- In vitro evaluation of APCs' targeting specificity, cellular uptake, phototoxicity, and penetration into multicellular tumor spheroids (MCTS).
Main Results:
- Successful synthesis of APCs with enhanced water solubility and strong near-infrared fluorescence in aqueous solutions.
- APCs demonstrated efficient singlet oxygen generation in solution and within cells upon laser irradiation.
- APCs specifically targeted PTK7-overexpressing cancer cells, enabling tumor cell imaging and diagnosis.
- APCs exhibited enhanced phototoxicity against target cancer cells and showed efficient penetration into MCTS, leading to cell damage.
Conclusions:
- The developed aptamer-Pyro conjugate (APC) is a robust molecule with improved water solubility and selective tumor-targeting capabilities.
- APCs demonstrate potential as a penetrable agent for cancer photodynamic therapy, offering improved efficacy and reduced off-target effects.
- This conjugate represents a promising advancement in developing targeted and effective photodynamic agents for cancer treatment.
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