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Near-infrared-responsive GE11-CuS@Gal nanoparticles as an intelligent drug release system for targeting therapy
Qinghua Lan1, Shuanghu Wang2, Zhouming Chen3
1Department of Pharmacy, The Fifth Affiliated Hospital of Wenzhou Medical University, Lishui, 323000, China; Key Laboratory of Imaging Diagnosis and Minimally Invasive Intervention Research, The Fifth Affiliated Hospital of Wenzhou Medical University, Lishui, 323000, China.
Abstract:
Galangin (Gal) is a natural plant flavonoid. More and more evidence shows that Gal can achieve anti-tumor effects by regulating various mechanisms. However, its poor water solubility, low bioavailability, and insufficient lesion targeting limit its clinical application. To overcome these shortcomings, we designed and developed a mesoporous nanosystem (GE11-CuS) that actively located the target area and photo-controlled drug release, which promoted the rapid accumulation of drugs in tumor tissues under NIR irradiation, thus achieving positive effects against cancer. In this study, we explored the application of the Gal-loaded nanometer system (GE11-CuS@Gal) in the treatment of oral squamous cell carcinoma (OSCC) both in vitro and in vivo. The results exhibited that GE11-CuS@Gal had excellent targeting ability and could accumulate efficiently in tumor cells (HSC-3). Meanwhile, the temperature of GE11-CuS@Gal increasing rapidly under NIR illumination damaged the integrity of the carrier and allowed Gal molecules to escape from the pores of the nanoparticles. When the accumulation of Gal in the nidus reached a certain level, the intracellular ROS level could be significantly increased and the antioxidative stress pathway mediated by Nrf2/OH-1 was effectively blocked, to inhibit the growth and migration of tumors. In conclusion, the GE11-CuS improved the antitumor activity of Gal in the body, which laid a foundation for the treatment of OSCC with traditional Chinese medicine ingredients.
Insights
This study developed a novel nanocarrier (GE11-CuS@Gal) to enhance galangin (Gal) for oral cancer treatment. The system effectively targets tumors and releases galangin under near-infrared light, improving anti-cancer effects.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Galangin (Gal), a natural flavonoid, exhibits anti-tumor properties but faces limitations in solubility, bioavailability, and targeting.
- Developing effective drug delivery systems is crucial for overcoming these challenges and improving therapeutic outcomes.
Purpose of the Study:
- To design and evaluate a mesoporous nanosystem (GE11-CuS) for targeted delivery and photo-controlled release of galangin (Gal).
- To investigate the efficacy of the galangin-loaded nanocarrier (GE11-CuS@Gal) in treating oral squamous cell carcinoma (OSCC) in vitro and in vivo.
Main Methods:
- Fabrication of a mesoporous nanosystem (GE11-CuS) for galangin encapsulation.
- In vitro and in vivo evaluation of GE11-CuS@Gal targeting efficiency and drug release under near-infrared (NIR) irradiation.
- Assessment of cellular responses, including reactive oxygen species (ROS) generation and Nrf2/OH-1 pathway inhibition.
Main Results:
- GE11-CuS@Gal demonstrated excellent targeting and accumulation in OSCC cells (HSC-3).
- NIR irradiation triggered rapid nanoparticle degradation and galangin release, leading to increased intracellular ROS levels.
- The nanocarrier effectively inhibited tumor growth and migration by blocking the Nrf2/OH-1 antioxidative stress pathway.
Conclusions:
- The GE11-CuS nanosystem significantly enhances the anti-tumor activity of galangin in oral squamous cell carcinoma.
- This targeted, photo-controlled drug delivery approach holds promise for the clinical application of traditional Chinese medicine ingredients in cancer therapy.

