Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F

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Publikace nespadá pod Lékařskou fakultu, ale pod Farmaceutickou fakultu. Oficiální stránka publikace je na webu muni.cz.
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BREZANI Veronika BLONDEAU Nicolas KOTOUCEK Jan KLÁSKOVÁ Eva ŠMEJKAL Karel HOŠEK Jan MASKOVA Eliska KULICH Pavel PRACHYAWARAKORN Vilailak HEURTEAUX Catherine MASEK Josef

Rok publikování 2024
Druh Článek v odborném periodiku
Časopis / Zdroj ACS Omega
Fakulta / Pracoviště MU

Farmaceutická fakulta

Citace
www https://pubs.acs.org/doi/10.1021/acsomega.3c07380
Doi http://dx.doi.org/10.1021/acsomega.3c07380
Popis 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.
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