Incorporation of Perillyl Alcohol into Lipid-Based Nanocarriers Enhances the Antiproliferative Activity in Malignant Glioma Cells

Abstract

Perillyl alcohol (PA), a naturally existing monocyclic terpene related to limonene, is characterized by its poor aqueous solubility and very limited bioavailability. Its potential anti-cancer activity against malignant glioma has been reported. The aim was to develop PA-loaded lipid-based nanocarriers (LNCs), and to investigate their anti-cancer activity against two different brain cell lines. Non-medicated and PA-loaded LNCs were prepared and characterized. The mechanism of cytotoxic activity of PA was conducted using a molecular docking technique. The cell viabilities against A172 and ANGM-CSS cells were evaluated. The results revealed that the average particle size of the prepared LNCs ranged from 248.67 ± 12.42 to 1124.21 ± 12.77 nm, the polydispersity index was 0.418 ± 0.043–0.509 ± 0.064, while the zeta potential ranged from −36.91 ± 1.31 to −15.20 ± 0.96 mV. The molecular docking studies demonstrated that the drug had binding activity to human farnesyltransferase. Following exposure of the two glioblastoma cell lines to the PA-loaded nanoformulations, MTS assays were carried out, and the data showed a far lower half-maximal inhibitory concentration in both cell lines when compared to pure drug and non-medicated nanocarriers. These results indicate the potential in vitro antiproliferative activity of PA-loaded LNCs. Therefore, the prepared PA-loaded nanocarriers could be used to enhance drug delivery across the blood–brain barrier (BBB) in order to treat brain cancer, especially when formulated in a suitable dosage form. The size, surface charge, and lipid composition of the LNCs make them promising for drug delivery across the BBB. Detailed pharmacokinetic and pharmacodynamic assessments, including the evaluation of BBB penetration, are necessary to better understand the compound’s distribution and effects within the brain.

Fabrication and evaluation of ribavirin-loaded electrospun nanofibers as an antimicrobial wound dressing

“…The assessment of in-vitro cellular viability of ribavirin, CD and their combination was performed following 24 and 48-hour cellular exposure to the human fibroblast HFF-1 cells (ATCC- SCRC-1401). The evaluation of the metabolic activity of ribavirin was conducted using the modified method of Ahmed et al, (2023) , using the colorimetric MTS assay (cell Titer 96® Aqueous one solution cell proliferation assay, Promega, Southampton, UK). HFF-1 cells were sub-cultured in Dulbecco's modified eagle medium (DMEM) containing the following: streptomycin (100 μg/mL), FBS (10 % (v/v)), and penicillin (100 U/mL), which were brought from Sigma-Aldrich (St. Louis, MO, USA).…”