Nucleus‐Targeting Carbon Quantum Dots Assembled with Gambogic Acid via π–π Stacking for Cancer Therapy

Abstract

Chemotherapy combined with nanocarriers has received increased attention as a thriving strategy for tumor therapy. However, drug resistance (DR), poor circulation, and retention in cells are the main challenges of this therapy. Herein, a novel strategy is developed to target drug delivery via 𝝅-𝝅 stacking interactions to overcome DR and short circulation and retention in cells. Carbon quantum dots (CDs) and gambogic acid (GA) are assembled via a 𝝅-𝝅 stacking interaction, which increases the drug-loading capacity of CDs as well as the circulation and retention of GA-loaded CDs (CDs/GA). CDs/GA significantly inhibit cell proliferation because CDs enter the nucleus and avoid drug pump recognition. GA released from CDs/GA promotes apoptosis by inducing the production of reactive oxygen species via the mitochondrial pathway. As a result, the delivery system of CDs/GA via 𝝅-𝝅 stacking displays a significant therapeutic effect on hepatoma (HepG2) and cervical cancer (HeLa) cells. The mechanisms of DR and induction of apoptosis are further investigated. The results suggest that chemotherapy combined with CDs can facilitate the targeting of the nucleus, thereby inducing apoptosis via the mitochondrial pathway.

Highly Efficient Loading of Procaine on Water-Soluble Carbon Dots toward Long-Acting Anesthesia

“…Five mathematical models were used to fit the in vitro release data of PrC/Cys-CDs kinetically to investigate the release mechanism, including zero-order, first-order, Higuchiorder, Rigter-Pappas-order, and Bhaskar-order equation. 43 2.7. Cytotoxicity Analysis.…”

Advanced Nanosystems for Cancer Therapeutics: A Review

“…The release of gambogic acid could promote apoptosis by stimulating the formation of ROS via the mitochondrial pathway. 178 Several challenges of conventional photosensitizers such as poor photostability, low solubility, and possible aggregations restrict their application in photodynamic therapy; hence, studies have focused on designing advanced nanosystems with improved properties for targeted photodynamic cancer therapy. 179 For example, hematoporphyrin photosensitizerencapsulated carbon QDs with excellent water solubility were developed using a microwave heating technique.…”

“…In another study, to overcome the obstacles of chemotherapy such as drug resistance, poor circulation, and retention in cells, carbon QDs and gambogic acid were assembled through a π–π stacking interaction to obtain a nanosystem with efficient therapeutic effects on HepG2 (hepatoma) and HeLa (cervical) cancer cells. The release of gambogic acid could promote apoptosis by stimulating the formation of ROS via the mitochondrial pathway …”