期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 216, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.colsurfb.2022.112537
关键词
Agomelatine; Nanostructured lipid carriers; Enhanced antidepressant activity; Behavioral deficit; Inflammatory mediators
资金
- Riphah Academy of Research and Education, Pakistan
- Basic Science Research Program of the National Research Foundation of Korea (NRF) - Ministry of Science and ICT, Republic of Korea [NRF-2021R1F1A1064021]
- Medical Research Program of Handok Jeseok Foundation, Republic of Korea
The present study aimed to prepare and optimize agomelatine-loaded nanostructured lipid carriers (AGMNLCs) for enhanced in vivo antidepressant potential. The optimized AGM-NLCs showed favorable physicochemical properties and sustained drug release, leading to improved neuronal morphology and reduced inflammation in mice brain.
The present study was intended to prepare and optimize agomelatine-loaded nanostructured lipid carriers (AGMNLCs) for augmented in vivo antidepressant potential. AGM-NLCs were optimized on several parameters including cumulative hydrophilic-lipophilic balance of surfactants, proportions of solid and liquid lipids, total amounts of drug and surfactants. AGM-NLCs were assessed for their physicochemical properties, in vitro AGM release and in vivo antidepressant effects in mice model. The optimized AGM-NLCs demonstrated spherical morphology with average particle size of 99.8 +/- 2.6 nm, PDI of 0.142 +/- 0.017, zeta potential of - 23.2 +/- 1.2 mV and entrapment efficiency of 97.1 +/- 2.1%. Thermal and crystallinity studies depict amorphous nature of AGM after its incorporation into NLCs. AGM-NLCs exhibit a sustained drug release profile after initial 2 h. Mice treated with AGM-NLCs exhibited reduced immobility time in behavioral analysis. Furthermore, cresyl violet staining demonstrated an improved neuronal morphology and survival in AGM-NLCs group. The concentrations and the expression of inflammatory markers (TNF-alpha and COX-2) in mice brain were significantly reduced by AGM-NLCs. Taken together, therapeutic effectiveness of AGM was markedly augmented in AGM-NLCs and thereby they could be promising nanocarriers for the effective delivery of antidepressants to brain.
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