Intranasal delivery of topiramate nanoemulsion: Pharmacodynamic, pharmacokinetic and brain uptake studies.
Brain Drug Uptake Study
Intranasal Delivery
Nanoemulsion
Pharmacodynamic Study
Pharmacokinetic Study
Topiramate
Journal
International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127
Informations de publication
Date de publication:
30 Jul 2020
30 Jul 2020
Historique:
received:
06
05
2020
revised:
27
05
2020
accepted:
28
05
2020
pubmed:
6
6
2020
medline:
25
2
2021
entrez:
6
6
2020
Statut:
ppublish
Résumé
Epilepsy is the noncommunicable and chronic central nervous system disorder characterized by frequent, unprovoked seizures, or electrical disturbances in the brain. Topiramate is used as an antiepileptic drug for the treatment of partial onset seizures, generalized seizures and Lennox-Gastaut Syndrome. Topiramate, a BCS class II drug, has a relatively low bioavailability. It is also a substrate of P-glycoprotein and Blood Brain Barrier restricts its entry into the brain. This investigation was aimed to prepare O/W nanoemulsion delivery system of topiramate to improve its brain bioavailability. Topiramate loaded nanoemulsion was prepared by phase titration method. It was consisting of 2% w/w Capmul MCM C8, 32% w/w Tween 20:Carbitol (2:1) and 66% w/w water. It was characterized for globule size, viscosity, polydispersibility index, zeta potential, pH, conductivity values, transmittance and TEM. Pharmacodynamic, pharmacokinetic and brain drug uptake study was carried out using wistar albino rats post intranasal and oral administration. Topiramate loaded nanoemulsion was having a globule size of 4.73 ± 0.52 nm. It was stable for six months. Brain uptake of topiramate post intranasal administration of topiramate loaded nanoemulsion was significantly (P < 1.86 × 10
Identifiants
pubmed: 32502686
pii: S0378-5173(20)30470-1
doi: 10.1016/j.ijpharm.2020.119486
pii:
doi:
Substances chimiques
Anticonvulsants
0
Emulsions
0
Topiramate
0H73WJJ391
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
119486Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.