Berberine-loaded liquid crystalline nanoparticles inhibit non-small cell lung cancer proliferation and migration in vitro

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.

Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review

“…These techniques mainly include diverse novel drug delivery systems. For example, a study showed that berberine-loaded liquid crystalline nanoparticles (LCNs) could overcome the poor water solubility and improve the bioavailability of berberine [ 130 ]. Another study showed that berberine-loaded bioformulation of silver nanoparticles (AgNPs) showed enhancing cytotoxicity against breast cancer cells and decreasing drug loss during their circulation in the blood [ 128 ].…”

Overcoming Multidrug Resistance of Antibiotics via Nanodelivery Systems

“…Tetracycline resistance genes (63 tet genes reported) are the most common acquired resistance genes in both Gram-positive and Gram-negative clinical isolates, which encodes numerous efflux transporters [13]. Tetracycline resistance gene tet (63), which serves as an efflux pump, has been found in a multiresistance plasmid from S. aureus chicken isolates [14].…”

“…Generally, nanotechnology comprises all systems whose mechanical, chemical, and pharmacological effects are modified to become substantially distinct, leading to special procedures due to the nanosized array of particles [ 61 , 62 , 63 , 64 ]. Nanoparticles utilized as drug delivery carriers are typically 100 nm in at least one dimension and comprise disintegrating components such as organic polymers, lipids, and metals [ 65 , 66 , 67 , 68 ].…”

Evaluation of the Cytotoxic Activity and Anti-Migratory Effect of Berberine–Phytantriol Liquid Crystalline Nanoparticle Formulation on Non-Small-Cell Lung Cancer In Vitro

“…BP-LCNs were formulated via ultrasonication as described by Paudel et al [51], with slight modification. The modification in the method involved the solubilization of berberine hydrochloride (Merck, Kenilworth, NJ, USA) in phytantriol (Tokyo Chemical Industry, Tokyo, Japan), instead of monoolein, followed by dispersion in Poloxamer 407 (P407, Merck) surfactant solution to obtain the BP-LCN formulation.…”

“…Among the nanoparticle-based formulations, liquid crystalline nanoparticles (LCNs) have been gaining interest as nanocarrier systems for anti-cancer and anti-inflammatory drugs, owing to their potential to improve the bioavailability and stability of the incorporated drug [47]. Monoolein-based LCNs incorporating rutin, naringenin, and berberine have already shown effectiveness in terms of their anti-cancer activity against NSCLC in vitro [48][49][50][51]. However, the anticancer potential of berberine-incorporated phytantriol-based LCNs has not yet been investigated.…”