Enhanced brain penetration of pretomanid by intranasal administration of an oil-in-water nanoemulsion.
Nanomedicine (Lond)
; 13(9): 997-1008, 2018 05.
Article
em En
| MEDLINE
| ID: mdl-29790418
ABSTRACT
AIM:
To enhance the drug delivery to the brain with an oil-in-water nanoemulsion of pretomanid via intranasal (IN) administration. MATERIALS &METHODS:
The study involved 70 male Sprague-Dawley rats (160-180 g) that received either 20 mg/kg body weight (b.w.) a nanoemulsion or a 20 mg/kg b.w. of pretomanid in solution via the IN route. The drug was quantified by liquid chromatography-tandem mass spectrometry to investigate whole tissue-drug concentrations, and mass spectrometric imaging to visualize drug localization in the brain.RESULTS:
Nanoemulsion delivery concentrations of pretomanid in the brain reached peak concentrations (Cmax) of 12,062.3 ng/g that is significantly higher than the required therapeutic level. The mass spectrometric imaging analysis clearly showed a time dependent and uniform distribution in the brain.CONCLUSION:
The results of this study show that IN delivery of oil-in-water nanoemulsion may be very promising for targeting anatomical tuberculosis reservoirs, such as the brain.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Administração Intranasal
/
Emulsões
/
Nanopartículas
/
Nitroimidazóis
Limite:
Animals
Idioma:
En
Revista:
Nanomedicine (Lond)
Ano de publicação:
2018
Tipo de documento:
Article