Abstract
Non-small cell lung cancer (NSCLC) is reported to have a high incidence rate and is one of the most prevalent types of cancer contributing towards 85% of all incidences of lung cancer. Berberine is an isoquinoline alkaloid which offers a broad range of therapeutical and pharmacological actions against cancer. However, extremely low water solubility and poor oral bioavailability have largely restricted its therapeutic applications. To overcome these limitations, we formulated berberine-loaded liquid crystalline nanoparticles (LCNs) and investigated their in vitro antiproliferative and antimigratory activity in human lung epithelial cancer cell line (A549). 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), trypan blue staining, and colony forming assays were used to evaluate the anti-proliferative activity, while scratch wound healing assay and a modified Boyden chamber assay were carried out to determine the anti-migratory activity. We also investigated major proteins associated with lung cancer progression. The developed nanoparticles were found to have an average particle size of 181.3 nm with spherical shape, high entrapment efficiency (75.35%) and have shown sustained release behaviour. The most remarkable findings reported with berberine-loaded LCNs were significant suppression of proliferation, inhibition of colony formation, inhibition of invasion or migration via epithelial mesenchymal transition, and proliferation related proteins associated with cancer progression. Our findings suggest that anti-cancer compounds with the problem of poor solubility and bioavailability can be overcome by formulating them into nanotechnology-based delivery systems for better efficacy. Further in-depth investigations into anti-cancer mechanistic research will expand and strengthen the current findings of berberine-LCNs as a potential NSCLC treatment option.
Highlights
Lung cancer is one of the most prevalent malignant tumours of the respiratory system, with significantly high rates of incidence and mortality (Khani et al 2018)
The berberine-liquid crystalline nanoparticles (LCNs) were produced as a yellowish, cloudy dispersion mixture, whereas the blank MO-based LCNs (MO-LCNs) were presented as a white, cloudy dispersion
The molecular simulation of the bimolecular (BER-MO) and trimolecular (BER-MO-PF127) systems revealed similar energy stabilization patterns characterized by initial destabilization of the drug-excipient complexes along with stabilization of attractive van der Waals interactions reaching negative energy values of − 7.522 and − 25.343 kcal/mol, respectively (Table 2)
Summary
Lung cancer is one of the most prevalent malignant tumours of the respiratory system, with significantly high rates of incidence and mortality (Khani et al 2018). Lung cancer is responsible for about 30 out of every 100 cancer-related deaths (Siegel et al 2021). In 2020 alone, there were more than 2 million new cases of lung cancer. There were around 1.8 million deaths in the same year from lung cancer (Sung et al 2021). About 85% of all cases of lung cancer are found to be non-small cell lung cancer (NSCLC) (Malyla et al 2020). Pollution, urban development, and industrialization remain to be the leading causative factors for global incidences of lung
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