2024
Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F
BREZANI, Veronika, Nicolas BLONDEAU, Jan KOTOUCEK, Eva KLÁSKOVÁ, Karel ŠMEJKAL et. al.Základní údaje
Originální název
Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F
Autoři
BREZANI, Veronika, Nicolas BLONDEAU, Jan KOTOUCEK, Eva KLÁSKOVÁ, Karel ŠMEJKAL, Jan HOŠEK, Eliska MASKOVA, Pavel KULICH, Vilailak PRACHYAWARAKORN, Catherine HEURTEAUX a Josef MASEK
Vydání
ACS Omega, WASHINGTON, American Chemical Society, 2024, 2470-1343
Další údaje
Jazyk
angličtina
Typ výsledku
Článek v odborném periodiku
Stát vydavatele
Spojené státy
Utajení
není předmětem státního či obchodního tajemství
Odkazy
Impakt faktor
Impact factor: 4.100 v roce 2022
Organizační jednotka
Farmaceutická fakulta
UT WoS
001164649600001
Štítky
Příznaky
Mezinárodní význam, Recenzováno
Změněno: 16. 8. 2024 08:12, Mgr. Tereza Miškechová
Anotace
V originále
Stilbenes in food and medicinal plants have been described as potent antiphlogistic and antioxidant compounds, and therefore, they present an interesting potential for the development of dietary supplements. Among them, macasiamenene F (MF) has recently been shown to be an effective anti-inflammatory and cytoprotective agent that dampens peripheral and CNS inflammation in vitro. Nevertheless, this promising molecule, like other stilbenes and a large percentage of drugs under development, faces poor water solubility, which results in trickier in vivo administration and low bioavailability. With the aim of improving MF solubility and developing a form optimized for in vivo administration, eight types of conventional liposomal nanocarriers and one type of PEGylated liposomes were formulated and characterized. In order to select the appropriate form of MF encapsulation, the safety of MF liposomal formulations was evaluated on THP-1 and THP-1-XBlue-MD2-CD14 monocytes, BV-2 microglia, and primary cortical neurons in culture. Furthermore, the cellular uptake of liposomes and the effect of encapsulation on MF anti-inflammatory effectiveness were evaluated on THP-1-XBlue-MD2-CD14 monocytes and BV-2 microglia. MF (5 mol %) encapsulated in PEGylated liposomes with an average size of 160 nm and polydispersity index of 0.122 was stable, safe, and the most promising form of MF encapsulation keeping its cytoprotective and anti-inflammatory properties.
Návaznosti
GA22-03187S, projekt VaV |
| ||
GA23-04655S, projekt VaV |
|