Dissolving microneedles loaded with nimodipine for prevention of sleep disorders at a high altitude.
Pharm Dev Technol
; 29(5): 415-428, 2024 Jun.
Article
em En
| MEDLINE
| ID: mdl-38626316
ABSTRACT
Sleep disorders are one of the most common acute reactions on the plateau, which can cause serious complications. However, there is no effective and safe treatment currently available. Nimodipine (NMD) is a dihydropyridine calcium channel blocker with neuroprotective and vasodilating activity, mainly used for the treatment of ischemic brain injury. Commercial oral or injectable NMD formulations are not a good option for central neuron diseases due to their poor brain delivery. In this study, nimodipine dissolving microneedles (NDMNs) were prepared for the prevention of sleep disorders caused by hypoxia. NDMNs were composed of NMD and polyvinyl pyrrolidone (PVP) K90 with a conical morphology and high rigidity. After administration of NDMNs on the back neck of mice, the concentration of NMD in the brain was significantly higher than that of oral medication as was confirmed by the fluorescent imaging on mouse models. NDMNs enhanced cognitive function, alleviated oxidative stress, and improved the sleep quality of mice with high-altitude sleep disorders. The blockage of calcium ion overloading may be an important modulation mechanism. NDMNs are a promising and user-friendly formulation for the prevention of high-altitude sleep disorders.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
Transtornos do Sono-Vigília
/
Bloqueadores dos Canais de Cálcio
/
Nimodipina
Limite:
Animals
Idioma:
En
Revista:
Pharm Dev Technol
Assunto da revista:
FARMACIA
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
China