Journal
MOLECULES
Volume 27, Issue 14, Pages -Publisher
MDPI
DOI: 10.3390/molecules27144521
Keywords
galangin; beta-cyclodextrin; drug delivery; biocompatibility; cytotoxicity; caspase-3 pathway; MCF-7 cells; REF cells
Funding
- Deanship of Scientific Research, Qassim University
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The study evaluates a newly modified cyclodextrin derivative, water-soluble beta-cyclodextrin-epichlorohydrin (beta-CD), as a drug carrier to improve the solubility and bioavailability of galangin (GAL). In vitro tests showed that the GAL/beta-CD complex exhibited cytotoxic effects on cancer cells without affecting normal cells. In vivo experiments on mice demonstrated the lack of toxic effects on normal cells.
The purpose of this study was to evaluate the potential of a newly modified cyclodextrin derivative, water-soluble beta-cyclodextrin-epichlorohydrin (beta-CD), as an effective drug carrier to enhance the poor solubility and bioavailability of galangin (GAL), a poorly water-soluble model drug. In this regard, inclusion complexes of GAL/beta-CDP were prepared. UV-VIS spectrophotometry, Fourier-transform infrared spectroscopy (FTIR), X-ray crystallography (XRD), zeta potential analysis, particle size analysis, field emission scanning electron microscopy (FESEM), and transmission electron microscopy (TEM) were applied to characterize the synthesized GAL/beta-CD. Michigan Cancer Foundation-7 (MCF-7; human breast cancer cells) and rat embryo fibroblast (REF; normal cells) were employed to examine the in vitro cytotoxic effects of GAL/beta-CD using various parameters. The dye-based tests of MTT and crystal violet clearly exhibited that GAL/beta-CD-treated cells had a reduced proliferation rate, an influence that was not found in the normal cell line. The cells' death was found to follow apoptotic mechanisms, as revealed by the dye-based test of acridine orange/ethidium bromide (AO/EtBr), with the involvement of the mitochondria via caspase-3-mediated events, as manifested by the Rh 123 test. We also included a mouse model to examine possible in vivo toxic effects of GAL/beta-CD. It appears that the inclusion complex does not have a significant influence on normal cells, as indicated by serum levels of kidney and liver enzymatic markers, as well as thymic and splenic mass indices. A similar conclusion was reached on the histological level, as manifested by the absence of pathological alterations in the liver, kidney, thymus, spleen, heart, and lung.
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