Graphene Oxide–PEG–Protocatechuic Acid Nanocomposite Formulation with Improved Anticancer Properties

• Main Authors: Bullo Saifullah, Kalaivani Buskaran, Rabia Baby Shaikh, Farahnaz Barahuie, Sharida Fakurazi, Mohd Aris Mohd Moklas, Mohd Zobir Hussein
• Format: Article
• Language: English
• Published: MDPI AG 2018-10-01
• Series: Nanomaterials
• Subjects: graphene oxide; PEG; cancer; drug delivery; protocatechuic acid; liver cancer; colon cancer
• Online Access: http://www.mdpi.com/2079-4991/8/10/820

The treatment of cancer through chemotherapy is limited by its toxicity to healthy tissues and organs, and its inability to target the cancer site. In this study, we have designed an anticancer nanocomposite delivery system for protocatechuic acid (PCA) using graphene oxide–polyethylene glycol as the nanocarrier, and coated with folic acid (GO–PEG–PCA–FA) for targeting the cancer cells. The designed anticancer delivery system was found to show much better anticancer activity than the free drug PCA against liver cancer HEP-G2 cells and human colon cancer HT-29 cells; at same time, it was found to be less toxic to normal fibroblast 3T3 cells. The folate-coated anticancer delivery system was found to show better activity then the free drug and the uncoated anticancer delivery system. The in vitro release of the PCA was found to be sustained in human physiological pHs, i.e., blood pH 7.4 and intracellular lysosomal pH 4.8. These in vitro findings are highly encouraging for further in vivo evaluation studies.