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

J 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.

Basic information

Original name

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

Authors

BREZANI, Veronika, Nicolas BLONDEAU, Jan KOTOUCEK, Eva KLÁSKOVÁ, Karel ŠMEJKAL, Jan HOŠEK, Eliska MASKOVA, Pavel KULICH, Vilailak PRACHYAWARAKORN, Catherine HEURTEAUX and Josef MASEK

Edition

ACS Omega, WASHINGTON, American Chemical Society, 2024, 2470-1343

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

URL

Impact factor

Impact factor: 4.100 in 2022

Organization unit

Faculty of Pharmacy

DOI

http://dx.doi.org/10.1021/acsomega.3c07380

UT WoS

001164649600001

Abstract

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.

Links

GA22-03187S, research and development project

Name: Racionální design částicových polysacharidových systémů pro přívod léčiv s širokým spekterem biologické aktivity k terapii sliznic (Acronym: 22-03187S)

Investor: Czech Science Foundation

GA23-04655S, research and development project

Name: Role prenylace a glykosylace v protizánětlivé aktivitě a metabolismu přírodních fenolových látek

Investor: Czech Science Foundation, Role of prenylation and glycosylation patterns in anti-inflammatory activity and metabolism of natural phenolic compounds

Citovat

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. 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.

@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.

Detailed Information on Publication Record