期刊
MATERIALS
卷 13, 期 16, 页码 -出版社
MDPI
DOI: 10.3390/ma13163618
关键词
chrysin; 2-hydroxypropyl-beta-cyclodextrin; random methyl-beta-cyclodextrin; Caco-2 permeability; phase-solubility
类别
资金
- Romanian Ministry of Research and Innovation, CCDI-UEFISCDI [PN-III-P2-2.1-PED-2016-1644 (193PED/2017), PN-III-P2-2.1-PED-2019-3609, PN-III-P1-1.2-PCCDI-2017-0782/REGMED]
- European Union
- European Social Fund
- [EFOP-3.6.1-16-2016-00022]
- [GINOP-2.3.3-15-2016-00021]
Chrysin is a bioflavonoid that can be found in natural products such as honey and propolis, and it possesses several biological effects such as antioxidant, anti-inflammatory, and anti-cancer activity. However, it is poorly soluble in water, and its bioavailability is limited. The aim of this research is to investigate the chrysin solubilization capacity of different beta-cylcodextrin derivatives and compare their biological activities. Chrysin was complexed with beta-cyclodextrin (beta CD), hydroxypropyl-beta-, (HPBCD) sulfobutylether-beta-, (SBECD), and randomly-methylated-beta-cyclodextrin (RAMEB) by the lyophilization method in 1:1 and 1:2 molar ratios. The solubilities of the chrysin-cyclodextrin complexes were tested, and the solubilization abilities of cyclodextrins were studied by phase solubility experiments. The cytotoxicity of the complexes was measured by the MTT method, and the permeability enhancement was tested on Caco-2 monolayers. The solubility study showed that the complexes formed with RAMEB had the highest solubility in water. The phase solubility experiments confirmed the strongest interaction between RAMEB and chrysin. In the viability test, none of the complexes showed cytotoxicity up to 100 mu M concentration. The permeability study revealed that both at 1:1 and 1:2 ratios, the RAMEB complexes were the most effective to enhance chrysin permeability through the Caco-2 monolayers. In conclusion, cyclodextrins, especially RAMEB, are suitable for improving chrysin solubility and absorption.
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