Piperine-loaded nanoparticles with enhanced dissolution and oral bioavailability for epilepsy control.
Eur J Pharm Sci
; 137: 104988, 2019 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-31291598
ABSTRACT
Piperine, an alkaloid from black pepper, has demonstrated beneficial effects in central nervous system, especially in epilepsy control. However, its therapeutic application remains limited due to the low aqueous solubility of piperine. Thus, the present study aimed to formulate piperine into a more solubilized form to enhance its oral bioavailability and facilitate its development as a potential anti-epileptic treatment. The nanoprecipitation method was applied to prepare piperine nanoparticles, which were then examined under transmission electron microscopy. A spherical nanosized particle was obtained with small particle size (average particle size 130.20⯱â¯1.57â¯nm), narrow size distribution (polydispersity index 0.195⯱â¯0.002) and efficient entrapment (entrapment efficiency 92.2⯱â¯2.5%). Compared with the unformulated piperine, nanosized piperine had a much faster dissolution rate with 3 times higher accumulated drug release after 24â¯h. After oral administration at 3.5â¯mg/kg in rats, the nanosized piperine formulations could improve its oral bioavailability by 2.7-fold with 16 times higher concentrations in brain at 10â¯h postdosing. Moreover, the piperine nanoparticles exhibited effective protection against pentylenetetrazol-induced seizures in both zebrafish and mice. In summary, the present study provided a simple formulation strategy for oral administration of piperine to overcome its limitation in water solubility. The developed formulations could effectively enhance oral bioavailability of piperine with promising anti-epileptic effect, which could be applied as a potential therapy in epilepsy control.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Contexto en salud:
1_ASSA2030
Problema de salud:
1_doencas_nao_transmissiveis
Asunto principal:
Piperidinas
/
Alcaloides
/
Epilepsia
/
Benzodioxoles
/
Alcamidas Poliinsaturadas
/
Nanopartículas
/
Anticonvulsivantes
Límite:
Animals
Idioma:
En
Revista:
Eur J Pharm Sci
Asunto de la revista:
FARMACIA
/
FARMACOLOGIA
/
QUIMICA
Año:
2019
Tipo del documento:
Article