Niosomal Formulation of a Lipoyl-Carnosine Derivative Targeting TRPA1 Channels in Brain.
TRPA1 antagonist
blood brain barrier
cortical spreading depression
niosomes
Journal
Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003
Informations de publication
Date de publication:
10 Dec 2019
10 Dec 2019
Historique:
received:
15
11
2019
revised:
04
12
2019
accepted:
06
12
2019
entrez:
15
12
2019
pubmed:
15
12
2019
medline:
15
12
2019
Statut:
epublish
Résumé
The transient receptor potential akyrin type-1 (TRPA1) is a non-selective cation channel playing a pivotal role in pain sensation and neurogenic inflammation. TRPA1 channels expressed in the central nervous system (CNS) have a critical role in the modulation of cortical spreading depression (CSD), which is a key pathophysiological basis of migraine pain. ADM_09 is a recently developed lipoic acid-based TRPA1 antagonist that is able to revert oxaliplatin-induced neuropathic pain and inflammatory trigeminal allodynia. In this context, aiming at developing drugs that are able to target TRPA1 channels in the CNS and promote an antioxidant effect, permeability across the blood-brain barrier (BBB) represents a central issue. Niosomes are nanovesicles that can be functionalized with specific ligands selectively recognized by transporters expressed on the BBB. In this work, the activity of ADM_09 on neocortex cultures was studied, and an efficient formulation to cross the BBB was developed with the aim of increasing the concentration of ADM_09 into the brain and selectively delivering it to the CNS rapidly after parenteral administration.
Identifiants
pubmed: 31835593
pii: pharmaceutics11120669
doi: 10.3390/pharmaceutics11120669
pmc: PMC6956366
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Ente Cassa di Risparmio di Firenze
ID : 2017.0726
Organisme : Ministero dell'Istruzione, dell'Università e della Ricerca
ID : Progetto Dipartimenti di Eccellenza 2018-2022
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