Ganoderenic acid D-loaded functionalized graphene oxide-based carrier for active targeting therapy of cervical carcinoma

• Published in: Biomedicine & pharmacotherapy Vol. 164; p. 114947
• Main Authors: Lu, Jiahui, Zhang, Anqiang, Zhang, Fuming, Linhardt, Robert J., Zhu, Zhihui, Yang, Yanzi, Zhang, Tinghuang, Lin, Zhibin, Zhang, Su, Zhao, Huajun, Sun, Peilong
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 01.08.2023; Elsevier
• Subjects: Active targeting antitumor; Cervical carcinoma; Ganoderenic acid D; Ganoderenic acid D; Active targeting antitumor; Cervical carcinoma
• ISSN: 0753-3322; 1950-6007
• DOI: 10.1016/j.biopha.2023.114947

Ganoderenic acid D (GAD), extracted from the Chinese herb Ganoderma lucidum, was loaded onto a graphene oxide-polyethylene glycol-anti-epidermal growth factor receptor (GO-PEG-EGFR) carrier to develop a targeting antitumor nanocomposite (GO-PEG@GAD). The carrier was fabricated from PEG and anti-EGFR aptamer modified GO. Targeting was mediated by the grafted anti-EGFR aptamer, which targets the membrane of HeLa cells. Physicochemical properties were characterized by transmission electron microscopy, dynamic light scattering, X-ray powder diffraction, and Fourier transform infrared spectroscopy. High loading content (77.3 % ± 1.08 %) and encapsulation efficiency (89.1 % ± 2.11 %) were achieved. Drug release continued for approximately 100 h. The targeting effect both in vitro and in vivo was confirmed by confocal laser scanning microscopy (CLSM) and imaging analysis system. The mass of the subcutaneous implanted tumor was significantly decreased by 27.27 ± 1.23 % after treatment with GO-PEG@GAD compared with the negative control group. Moreover, the in vivo anti-cervical carcinoma activity of this medicine was due to activation of the intrinsic mitochondrial pathway. •Active targeting to cervical carcinoma was achieved through coupling the anti-epidermal growth factor receptor (EGFR) aptamer.•The side effects of Ganoderenic acid D (GAD) on the major organs could be reduced after packaged.•In vivo anti-cervical carcinoma mechanism of GO-PEG@GAD was mainly through activating the intrinsic mitochondrial pathway.