Effects of Microencapsulated Ferulic Acid or Its Prodrug Methyl Ferulate on Neuroinflammation Induced by Muramyl Dipeptide
Giada Botti,
Anna Bianchi,
Barbara Pavan (),
Paola Tedeschi,
Valentina Albanese,
Luca Ferraro,
Federico Spizzo,
Lucia Del Bianco and
Alessandro Dalpiaz
Additional contact information
Giada Botti: Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, via Fossato di Mortara 19, I-44121 Ferrara, Italy
Anna Bianchi: Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, via Fossato di Mortara 19, I-44121 Ferrara, Italy
Barbara Pavan: Department of Neuroscience and Rehabilitation—Section of Physiology, University of Ferrara, via L. Borsari 46, I-44121 Ferrara, Italy
Paola Tedeschi: Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, via Fossato di Mortara 19, I-44121 Ferrara, Italy
Valentina Albanese: Department of Environmental and Prevention Sciences, University of Ferrara, Corso Ercole I d’Este 32, I-44121 Ferrara, Italy
Luca Ferraro: Department of Life Sciences and Biotechnology, University of Ferrara and LTTA Center, via Fossato di Mortara 19, I-44121 Ferrara, Italy
Federico Spizzo: Department of Physics and Earth Science, University of Ferrara, via G. Saragat 1, I-44122 Ferrara, Italy
Lucia Del Bianco: Department of Physics and Earth Science, University of Ferrara, via G. Saragat 1, I-44122 Ferrara, Italy
Alessandro Dalpiaz: Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, via Fossato di Mortara 19, I-44121 Ferrara, Italy
IJERPH, 2022, vol. 19, issue 17, 1-24
Abstract:
Ferulic acid (Fer) is known for its antioxidant and anti-inflammatory activities, which are possibly useful against neurodegenerative diseases. Despite the ability of Fer to permeate the brain, its fast elimination from the body does not allow its therapeutic use to be optimized. The present study proposes the preparation and characterization of tristearin- or stearic acid-based solid lipid microparticles (SLMs) as sustained delivery and targeting systems for Fer. The microparticles were produced by conventional hot emulsion techniques. The synthesis of the methyl ester of Fer (Fer-Me) allowed its encapsulation in the SLMs to increase. Fer-Me was hydrolyzed to Fer in rat whole blood and liver homogenate, evidencing its prodrug behavior. Furthermore, Fer-Me displayed antioxidant and anti-inflammatory properties. The amount of encapsulated Fer-Me was 0.719 ± 0.005% or 1.507 ± 0.014% in tristearin or stearic acid SLMs, respectively. The tristearin SLMs were able to control the prodrug release, while the stearic acid SLMs induced a significant increase of its dissolution rate in water. Jointly, the present results suggest that the tristearin SLMs loaded with Fer-Me could be a potential formulation against peripheral neuropathic pain; conversely, the stearic acid SLMs could be useful for Fer-Me uptake in the brain after nasal administration of the formulation.
Keywords: ferulic acid; methyl ferulate; prodrug; antioxidant; solid lipid microparticles; inflammation; TNF-α (search for similar items in EconPapers)
JEL-codes: I I1 I3 Q Q5 (search for similar items in EconPapers)
Date: 2022
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