Related Experiment Video
Updated: Sep 28, 2025
Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles
Published on: December 1, 2016
Targeted delivery of quercetin by biotinylated mixed micelles for non-small cell lung cancer treatment
Kangkang Li1, Xinlong Zang1, Xiangjun Meng2
1School of Basic Medicine, Qingdao University,Qingdao, China.
Abstract:
Lung cancer is the leading cause of cancer death world-wide and its treatment remains a challenge in clinic, especially for non-small cell lung cancer (NSCLC). Thus, more effective therapeutic strategies are required for NSCLC treatment. Quercetin (Que) as a natural flavonoid compound has gained increasing interests due to its anticancer activity. However, poor water solubility, low bioavailability, short half-life, and weak tumor accumulation hinder in vivo applications and antitumor effects of Que. In this study, we developed Que-loaded mixed micelles (Que-MMICs) assembled from 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol)-biotin (DSPE-PEG-biotin) and poly(ethylene glycol) methyl ether methacrylate-poly[2-(dimethylamino) ethyl acrylate]-polycaprolactone (PEGMA-PDMAEA-PCL) for NSCLC treatment. The results showed that Que was efficiently encapsulated into the mixed micelles and the encapsulation efficiency (EE) was up to 85.7%. Cellular uptake results showed that biotin conjugation significantly improved 1.2-fold internalization of the carrier compared to that of non-targeted mixed micelles. In vitro results demonstrated that Que-MMICs could improve cytotoxicity (IC50 = 7.83 μg/mL) than Que-MICs (16.15 μg/mL) and free Que (44.22 μg/mL) to A549 cells, which efficiently induced apoptosis and arrested cell cycle. Furthermore, Que-MMICs showed satisfactory tumor targeting capability and antitumor efficacy possibly due to the combination of enhanced permeability and retention (EPR) and active targeting effect. Collectively, Que-MMICs demonstrated high accumulation at tumor site and exhibited superior anticancer activity in NSCLC bearing mice model.
Insights
Researchers developed quercetin-loaded mixed micelles (Que-MMICs) to improve non-small cell lung cancer (NSCLC) treatment. These micelles enhance quercetin delivery, showing superior anticancer effects and tumor targeting in preclinical models.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Lung cancer, particularly non-small cell lung cancer (NSCLC), is a leading cause of cancer mortality, necessitating advanced therapeutic strategies.
- Quercetin (Que), a natural flavonoid, exhibits anticancer properties but faces limitations in solubility, bioavailability, and tumor accumulation for effective in vivo application.
- Developing novel drug delivery systems is crucial to overcome these challenges and enhance the therapeutic efficacy of natural compounds like quercetin.
Purpose of the Study:
- To develop and characterize quercetin-loaded mixed micelles (Que-MMICs) for improved non-small cell lung cancer (NSCLC) treatment.
- To evaluate the enhanced cellular uptake, cytotoxicity, and antitumor efficacy of Que-MMICs compared to free quercetin.
- To investigate the potential of biotin-conjugated nanoparticles for targeted drug delivery in NSCLC.
Main Methods:
- Fabrication of Que-MMICs using DSPE-PEG-biotin and PEGMA-PDMAEA-PCL polymers.
- Quantification of quercetin encapsulation efficiency (EE).
- Assessment of cellular uptake via flow cytometry, in vitro cytotoxicity assays (IC50 determination), cell cycle analysis, and apoptosis assays.
- Evaluation of in vivo antitumor efficacy and tumor targeting in a murine model.
Main Results:
- Que-MMICs achieved a high encapsulation efficiency of 85.7% for quercetin.
- Biotin conjugation significantly enhanced cellular internalization (1.2-fold) compared to non-targeted micelles.
- Que-MMICs exhibited superior in vitro cytotoxicity against A549 lung cancer cells (IC50 = 7.83 μg/mL) compared to free Que (44.22 μg/mL).
- Que-MMICs effectively induced apoptosis and cell cycle arrest, demonstrating significant antitumor efficacy and tumor accumulation in vivo.
Conclusions:
- Que-MMICs represent a promising nanocarrier system for enhancing the therapeutic potential of quercetin in NSCLC treatment.
- The biotin-targeted delivery system effectively improves drug internalization and antitumor activity.
- These findings support the development of advanced nanomedicines for overcoming drug delivery challenges in cancer therapy.
