Abstract
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.
Highlights
The emergence of the nanomedicine is one of the most significant advancements in the field of medical science in this century
The dynamic light scattering (DLS) technique was used for the analysis of the particle size distribution of the anticancer nanocomposite Graphene oxide (GO)–Polyethylene glycol (PEG)–protocatechuic acid (PCA)–folic acid (FA) using a Zetasizer
The designed anticancer nanocomposite GO with polyethylene glycol (GO–PEG)–PCA–FA and all of the other samples such as empty nanocarrier GO–PEG, free drug PCA, and nanocomposite without folic acid coating GO–PEG–PCA were found to be highly biocompatible with normal 3T3 cells
Summary
The emergence of the nanomedicine is one of the most significant advancements in the field of medical science in this century. The high affinity of the folate receptor that is preferentially expressed in cancer cells is rarely expressed in normal cells This has allowed the development of the targeted delivery of anticancer drugs at the cancer at the tumor sites to maximize anticancer efficacy with minimizing side effects to healthy tissues [42,43,44,45]. We have designed an anticancer nanocomposite formulation using GO–PEG as the nanocarrier loaded with anticancer drug PCA, and coated it with folic acid (FA) for the active targeting of the different cancer cells.
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