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@article{2381977,
author = {Brezani, Veronika and Blondeau, Nicolas and Kotoucek, Jan and Klásková, Eva and Šmejkal, Karel and Hošek, Jan and Maskova, Eliska and Kulich, Pavel and Prachyawarakorn, Vilailak and Heurteaux, Catherine and Masek, Josef},
article_location = {WASHINGTON},
article_number = {8},
doi = {http://dx.doi.org/10.1021/acsomega.3c07380},
language = {eng},
issn = {2470-1343},
journal = {ACS Omega},
title = {Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F},
url = {https://pubs.acs.org/doi/10.1021/acsomega.3c07380},
volume = {9},
year = {2024}
}
TY - JOUR
ID - 2381977
AU - Brezani, Veronika - Blondeau, Nicolas - Kotoucek, Jan - Klásková, Eva - Šmejkal, Karel - Hošek, Jan - Maskova, Eliska - Kulich, Pavel - Prachyawarakorn, Vilailak - Heurteaux, Catherine - Masek, Josef
PY - 2024
TI - Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F
JF - ACS Omega
VL - 9
IS - 8
SP - 9027-9039
EP - 9027-9039
PB - American Chemical Society
SN - 24701343
UR - https://pubs.acs.org/doi/10.1021/acsomega.3c07380
N2 - 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.
ER -
BREZANI, Veronika, Nicolas BLONDEAU, Jan KOTOUCEK, Eva KLÁSKOVÁ, Karel ŠMEJKAL, Jan HOŠEK, Eliska MASKOVA, Pavel KULICH, Vilailak PRACHYAWARAKORN, Catherine HEURTEAUX and Josef MASEK. Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F. \textit{ACS Omega}. WASHINGTON: American Chemical Society, 2024, vol.~9, No~8, p.~9027-9039. ISSN~2470-1343. Available from: https://dx.doi.org/10.1021/acsomega.3c07380.
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