Zhang Youwen, Zhu Yini, Kim Gaeun, Wang Ceming, Zhu Runyao, Lu Xin, Chang Hsueh-Chia, Wang Yichun
bioRxiv. 2023 Jan 20:2023.01.20.523510. doi: 10.1101/2023.01.20.523510.
As nanoscale extracellular vesicles secreted by cells, exosomes have enormous potential as safe and effective vehicles to deliver 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 π-π stacking and van der Waals interactions. 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.
作为细胞分泌的纳米级细胞外囊泡,外泌体作为将药物递送至损伤部位的安全有效载体具有巨大潜力。尽管基于外泌体的药物递送系统取得了令人鼓舞的进展,但外泌体载药仍存在挑战,这阻碍了外泌体的临床应用。在此,我们报告了一种基于与外泌体脂质双层手性匹配的外源性药物通用手性石墨烯量子点(GQDs)外泌体装载平台。疏水性和亲水性化学药物及生物药物均可通过π-π堆积和范德华相互作用功能化或吸附到GQDs上。通过调整配体和GQD尺寸以优化其手性,我们证明阿霉素和小干扰RNA(siRNA)的载药效率分别为66.3%和64.1%,显著高于其他报道的外泌体装载技术。