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A lipid droplet-targeted AIE photosensitizer for efficient multi-type ROS generation and breast cancer photodynamic
Yukun Zhang1, Lidong Deng2, Qiyan Li2
1School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640, PR China.
Abstract:
Photodynamic therapy (PDT) is a promising non-invasive strategy for breast cancer, yet its clinical translation is hindered by fluorescence quenching, insufficient reactive oxygen species (ROS) generation and poor tumor targeting. Herein, a novel lipid droplet-targeted aggregation-induced emission (AIE) photosensitizer CTC was designed and synthesized. CTC has a large Stokes shift of 150 nm to avoid self-absorption and exhibits typical AIE properties in aqueous environments. Under white light irradiation, it efficiently generates three cytotoxic ROS (1O2, ·OH, O2•-), with a high colocalization coefficient of 0.95 with lipid droplets in 4 T1 cells. CTC shows excellent biocompatibility in the dark and potent phototoxicity under illumination. In vivo, CTC combined with light significantly inhibits 4 T1 tumor growth without systemic toxicity. Density functional theory calculations elucidate its multi-type ROS generation mechanism, providing a novel candidate and new insight for safe and efficient breast cancer PDT.
Insights
A new photosensitizer targets lipid droplets for breast cancer photodynamic therapy (PDT). This approach enhances reactive oxygen species (ROS) generation and tumor targeting, showing significant tumor growth inhibition with minimal toxicity.
Area of Science:
- Biochemistry
- Nanotechnology
- Oncology
Background:
- Photodynamic therapy (PDT) shows promise for breast cancer treatment but faces challenges like fluorescence quenching and poor tumor targeting.
- Developing effective photosensitizers is crucial for advancing PDT clinical applications.
Purpose of the Study:
- To design and synthesize a novel lipid droplet-targeted aggregation-induced emission (AIE) photosensitizer for enhanced breast cancer PDT.
- To evaluate the efficacy and safety of the developed photosensitizer in vitro and in vivo.
Main Methods:
- Synthesis of a novel AIE photosensitizer (CTC) with a large Stokes shift.
- In vitro evaluation of ROS generation, cellular uptake, colocalization with lipid droplets, biocompatibility, and phototoxicity.
- In vivo studies in a 4T1 breast cancer mouse model to assess tumor growth inhibition and systemic toxicity.
- Density functional theory (DFT) calculations to elucidate the ROS generation mechanism.
Main Results:
- The synthesized CTC photosensitizer exhibits aggregation-induced emission (AIE) properties and a large Stokes shift.
- CTC efficiently generates three types of cytotoxic reactive oxygen species (ROS) upon white light irradiation.
- High colocalization (0.95) of CTC with lipid droplets in 4T1 cells was observed.
- CTC demonstrated excellent biocompatibility in the dark and potent phototoxicity under illumination.
- In vivo, CTC combined with light significantly inhibited 4T1 tumor growth without causing systemic toxicity.
Conclusions:
- The novel lipid droplet-targeted AIE photosensitizer CTC offers a promising strategy for safe and efficient breast cancer PDT.
- CTC overcomes key limitations of traditional PDT, including fluorescence quenching and poor targeting.
- This study provides new insights into multi-type ROS generation mechanisms for improved cancer therapy.
