Liposomal Formulation Improves the Bioactivity of Usnic Acid in RAW 264.7 Macrophage Cells Reducing its Toxicity.
Usnic acid
antioxidant
bioactive enhancement
drug delivery
liposomes
macrophages
Journal
Current drug delivery
ISSN: 1875-5704
Titre abrégé: Curr Drug Deliv
Pays: United Arab Emirates
ID NLM: 101208455
Informations de publication
Date de publication:
2024
2024
Historique:
received:
10
06
2022
revised:
13
10
2022
accepted:
08
11
2022
pubmed:
12
1
2023
medline:
12
1
2023
entrez:
11
1
2023
Statut:
ppublish
Résumé
Reactive oxygen species (ROS) production and oxidative stress may be responsible for the onset of several chronic diseases. Usnic acid (UA) is a natural secondary metabolite of lichens with several healthful bioactivities, including antioxidant properties. However, UA is a hydrophobic compound known for its hepatic toxicity. These aspects limit its therapeutic applications. To overcome these drawbacks and improve the pharmacological use of hydrophobic compounds, nanotechnology is widely used. Therefore, the incorporation of UA into appropriate nanocarriers could enhance the bioactivity of UA by increasing its solubility. The aim of this work was to improve the solubility of UA and its bioactivity in the absence of cytotoxicity. In this study, UA loaded liposomes (UA-LP) were developed. The formulations were chemically and physically characterized, and an in vitro release study was performed. Free UA and UA-LP were tested on RAW 264.7 murine macrophages in terms of cytotoxicity, intracellular ROS production, and NO release in the absence or presence of pro-oxidant LPS stimulus. UA-LP showed excellent physical and chemical stability during storage and improved solubility of UA. UA-LP showed an antioxidant effect in the absence of cytotoxicity compared with free UA on LPS-exposed macrophages. For the first time, liposomal formulation improved the beneficial action of UA in terms of solubility and antioxidant activity.
Sections du résumé
BACKGROUND
BACKGROUND
Reactive oxygen species (ROS) production and oxidative stress may be responsible for the onset of several chronic diseases. Usnic acid (UA) is a natural secondary metabolite of lichens with several healthful bioactivities, including antioxidant properties. However, UA is a hydrophobic compound known for its hepatic toxicity. These aspects limit its therapeutic applications. To overcome these drawbacks and improve the pharmacological use of hydrophobic compounds, nanotechnology is widely used. Therefore, the incorporation of UA into appropriate nanocarriers could enhance the bioactivity of UA by increasing its solubility.
OBJECTIVE
OBJECTIVE
The aim of this work was to improve the solubility of UA and its bioactivity in the absence of cytotoxicity.
METHODS
METHODS
In this study, UA loaded liposomes (UA-LP) were developed. The formulations were chemically and physically characterized, and an in vitro release study was performed. Free UA and UA-LP were tested on RAW 264.7 murine macrophages in terms of cytotoxicity, intracellular ROS production, and NO release in the absence or presence of pro-oxidant LPS stimulus.
RESULTS
RESULTS
UA-LP showed excellent physical and chemical stability during storage and improved solubility of UA. UA-LP showed an antioxidant effect in the absence of cytotoxicity compared with free UA on LPS-exposed macrophages.
CONCLUSION
CONCLUSIONS
For the first time, liposomal formulation improved the beneficial action of UA in terms of solubility and antioxidant activity.
Identifiants
pubmed: 36631924
pii: CDD-EPUB-128748
doi: 10.2174/1567201820666230111112415
doi:
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
91-103Subventions
Organisme : Florence University of the Arts
Informations de copyright
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