Title:TPGS-modified Chitosan Nanoparticles of EGFR Inhibitor: Physicochemical
and In vitro Evaluation against HepG2 Cell Lines
Volume: 22
Issue: 4
Author(s): Mahendra Singh, Alka, Prashant Shukla, Zhi-Hong Wen, Chou-Yuan Ko*Ramachandran Vinayagam*
Affiliation:
- Division of Gastroenterology and Hepatology, Department of Internal Medicine,
Kaohsiung Armed Forces General Hospital, Kaohsiung 80284, Taiwan
- Institute of Medical Science and Technology,
National Sun Yat-sen University, Kaohsiung 80424, Taiwan
- Department of Biotechnology, Institute of Biotechnology, Life and Applied Sciences, Yeungnam University, Gyeongsan,
Gyeongbuk 38541, Republic of Korea
Keywords:
Gefitinib, hepatocellular carcinoma, chitosan, nanoparticles, nanomedicine, HepG2, cytotoxicity.
Abstract:
Background: Gefitinib (GFN) is an Epithelial Growth Factor Receptor (EGFR) inhibitor,
and Food and Drug Administration (FDA) has approved medication to treat lung cancer. However,
this investigation aimed to produce and characterize Gefitinib (GFN)-loaded chitosan and soy lecithin
nanoparticles (NPs) modified with D-α-tocopheryl polyethylene glycol 1000 succinate mono ester
(TPGS) and assess their therapeutic potential against HepG2 liver cell lines.
Methods: Chitosan, a cationic polymer with biocompatible and biodegradable properties, was combined
with soy lecithin to develop the NPs loaded with GFN using a self-organizing ionic interaction
methodology.
Results: The entrapment efficiency and drug loading were found to be 59.04±4.63 to 87.37±3.82%
and 33.46±3.76 to 49.50±4.35%, respectively, and results indicated the encapsulation of GEN in NPs.
The pH of the formulations was observed between 4.48-4.62. Additionally, all the prepared NPs
showed the size and PDI range of 89.2±15.9 nm to 799.2±35.8 nm and 0.179±0.065 to 0.455±0.097,
respectively. The FTIR bands in optimized formulation (GFN-NP1) indicated that the drug might be
contained within the NP's core. The SEM photograph revealed the spherical shape of NPs. The kinetic
release model demonstrated the combination of diffusion and erosion mechanisms. The IC50 value
of GFN and GFN-NP1 formulation against the HepG2 cell lines were determined and found to be
63.22±3.36 μg/ml and 45.80±2.53 μg/ml, respectively. DAPI and PI staining agents were used to
detect nuclear morphology.
Conclusion: It was observed that the optimized GFN-NP1 formulation successfully internalized and
inhibited the growth of HepG2 cells. Hence, it can be concluded that the prepared NPs can be a new
therapeutic option for treating liver cancer.
