scholarly journals Morphological Changes and Cellular Uptake of Functionalized Graphene Oxide Loaded with Protocatechuic Acid and Folic Acid in Hepatocellular Carcinoma Cancer Cell

2020 ◽  
Vol 21 (16) ◽  
pp. 5874
Author(s):  
Kalaivani Buskaran ◽  
Mohd Zobir Hussein ◽  
Mohamad Aris Mohd Moklas ◽  
Sharida Fakurazi

The development of nanocomposites has swiftly changed the horizon of drug delivery systems in defining a new platform. Major understanding of the interaction of nanocomposites with cells and how the interaction influences intracellular uptake is an important aspect to study in order to ensure successful utilisation of the nanocomposites. Studies have suggested that the nanocomposites’ ability to permeate into biological cells is attributable to their well-defined physicochemical properties with nanoscale size, which is relevant to the nanoscale components of biology and cellular organelles. The functionalized graphene oxide coated with polyethylene glycol, loaded with protocatechuic acid and folic acid (GOP-PCA-FA) nanocomposite intracellular uptake was analysed using transmission electron microscope. The accumulation of fluorescent-labelled nanocomposites in the HepG2 cell was also analysed using a fluorescent microscope. In vitro cellular uptake showed that there was uptake of the drug from 24 h into the cells and the release study using fluorescently tagged nanocomposite demonstrated that release and accumulation were observed at 24 h and 48 h. Moreover, the migration ability of tumor cells is a key step in tumor progression which was observed 48 h after treatment. The GOP serves as a potential nanocarrier system which is capable of improving the therapeutic efficacy of drugs and biomolecules in medical as well as pharmaceutical applications through the enhanced intracellular release and accumulation of the encapsulated drugs. Nonetheless, it is essential to analyse the translocation of our newly developed GOP-PCA-FA, and its efficiency for drug delivery, effective cellular uptake, and abundant intracellular accumulation would be compromised by possible untoward side effects.

Materials ◽  
2021 ◽  
Vol 14 (4) ◽  
pp. 817
Author(s):  
Kalaivani Buskaran ◽  
Saifullah Bullo ◽  
Mohd Zobir Hussein ◽  
Mas Jaffri Masarudin ◽  
Mohamad Aris Mohd Moklas ◽  
...  

Liver cancer is listed as the fifth-ranked cancer, responsible for 9.1% of all cancer deaths globally due to its assertive nature and poor survival rate. To overcome this obstacle, efforts have been made to ensure effective cancer therapy via nanotechnology utilization. Recent studies have shown that functionalized graphene oxide (GO)-loaded protocatechuic acid has shown some anticancer activities in both passive and active targeting. The nanocomposites’ physicochemical characterizations were conducted. A lactate dehydrogenase experiment was conducted to estimate the severity of cell damage. Subsequently, a clonogenic assay was carried out to examine the colony-forming ability during long-term exposure of the nanocomposites. The Annexin V/ propidium iodide analysis showed that nanocomposites induced late apoptosis in HepG2 cells. Following the intervention of nanocomposites, cell cycle arrest was ascertained at G2/M phase. There was depolarization of mitochondrial membrane potential and an upregulation of reactive oxygen species when HepG2 cells were induced by nanocomposites. Finally, the proteomic profiling array and quantitative reverse transcription polymerase chain reaction revealed the expression of pro-apoptotic and anti-apoptotic proteins induced by graphene oxide conjugated PEG loaded with protocatechuic acid drug folic acid coated nanocomposite (GOP–PCA–FA) in HepG2 cells. In conclusion, GOP–PCA–FA nanocomposites treated HepG2 cells exhibited significant anticancer activities with less toxicity compared to pristine protocatechuic acid and GOP–PCA nanocomposites, due to the utilization of a folic acid-targeting nanodrug delivery system.


2018 ◽  
Vol 1 (2) ◽  
pp. 922-932 ◽  
Author(s):  
Marcelo de Sousa ◽  
Luis Augusto Visani de Luna ◽  
Leandro Carneiro Fonseca ◽  
Selma Giorgio ◽  
Oswaldo Luiz Alves

2020 ◽  
Vol 8 ◽  
Author(s):  
Livia E. Sima ◽  
Gabriela Chiritoiu ◽  
Irina Negut ◽  
Valentina Grumezescu ◽  
Stefana Orobeti ◽  
...  

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