Chiral Graphene Quantum Dots Enhanced Drug Loading into Exosomes

Abstract

As nanoscale extracellular vesicles secreted by cells, exosomes have enormous potential as safe and effective vehicles to delivery drugs into lesion locations. Despite promising advances with exosome-based drug delivery systems, there are still challenges to drug loading into exosome, which hinder the clinical applications of exosomes. Herein, we report an exogenous drug-agnostic chiral graphene quantum dots (GQDs) exosome-loading platform, based on chirality matching with the exosome lipid bilayer. Both hydrophobic and hydrophilic chemical and biological drugs can be functionalized or adsorbed onto GQDs by pi stacking and van der Waals interactions, respectively. By tuning the ligands and GQD size to optimize its chirality, we demonstrate drug loading efficiency of 66.3% and 64.1% for Doxorubicin and siRNA, which is significantly higher than other reported exosome loading techniques.

A Panorama of Extracellular Vesicle Applications: From Biomarker Detection to Therapeutics

“…Passive loading methods are useful for only a subset of drugs, although a recent study suggests that graphene quantum dots that match the chirality of the EV bilayer could permit drug-agnostic loading of hydrophilic and hydrophobic small molecule and biologic drugs at high efficiency. 75 MSCderived EVs are also frequently used in drug delivery applications 76 due to their history of safe use, but significant care must be taken to maintain them in their undifferentiated state. Substantial effort has thus been focused on developing stable cell lines suitable for use in EV drug delivery applications.…”

Strategic Assessment of Boron-Enriched Carbon Dots/Naproxen: Diagnostic, Toxicity, and In Vivo Therapeutic Evaluation

“…25,26 Conversely, chemical conjugation with polymer materials provides advantages such as hydrophobic drug solubility, controlled pharmacokinetics, and reduced drug release in large quantities. 27,28 A previous study evaluated tetrazine-functionalized boron-rich carbon dots, which demonstrated rapid clearance and low tumor absorption following intravenous administration in a mouse HER2-positive tumor model. 29 Naproxen, a widely recognized nonsteroidal anti-inflammatory drug (NSAID), has recently garnered attention for its potential anticancer properties, as evidenced by its efficacy as a COX-2 inhibitor in clinical trials.…”

Novel rod‐like carbon nanomaterials as near infrared‐responsive drug delivery system for potential anticancer applications

“…The general treatments of cancer include surgery [1,2], chemotherapy [3,4], radiotherapy [5,6], and so on. With the rapid development of nanotechnology and materials science [7][8][9][10], nano-drug delivery systems [11][12][13][14] have been widely concerned in the cancers' diagnosis [15] and treatment [16]. Among them, carbon nanomaterials have attracted extensive attention due to excel-lent water solubility, high biocompatibility, and low toxicity.…”