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Folic Acid-Modified Cyclodextrin Multivalent Supramolecular Assembly for Photodynamic Therapy
Xianyin Dai1, Man Huo1, Bing Zhang2
1College of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China.
Biomacromolecules
|August 3, 2022
Summary
Researchers developed adaptive supramolecular nanoparticles for dual-organelle targeting in cancer therapy. These nanoparticles selectively accumulate in cancer cell mitochondria and lysosomes, achieving 99% cancer cell ablation via photodynamic therapy.
Area of Science:
- Biomaterials Science
- Supramolecular Chemistry
- Nanotechnology
Background:
- Supramolecular assemblies with photoluminescence and biological functions are crucial in biomaterials.
- Developing targeted therapies for cancer cell ablation remains a significant challenge.
Purpose of the Study:
- To create an adaptive supramolecular assembly for dual-organelle targeted photodynamic cancer cell ablation.
- To investigate the targeted delivery and therapeutic efficacy of novel nanoparticles.
Main Methods:
- A two-stage co-assembly strategy using adamantane-connected pyrenyl pyridinium derivative (APA2), sulfonated aluminum phthalocyanine (PcS), and folic acid-modified β-cyclodextrin (FA-CD).
- Characterization of nanoparticle formation, size, and cellular uptake via endocytosis in HeLa and 293T cells.
- In situ tracking of nanoparticle disaggregation and accumulation in mitochondria and lysosomes within cancer cells.
Main Results:
- Spherical nanoparticles (approx. 50 nm) were formed with targeted uptake by HeLa cancer cells.
- Nanoparticles adaptively disaggregated intracellularly, selectively targeting mitochondria and lysosomes.
- Efficient singlet oxygen generation under light irradiation led to up to 99% cancer cell ablation.
Conclusions:
- The developed adaptive supramolecular multivalent assembly offers a feasible strategy for precise organelle-targeted imaging.
- This approach provides an efficient, synergistic photodynamic effect for in situ cancer cell ablation.
- The study highlights the potential of adaptive nanomaterials in advanced cancer therapy.

