Intranasal delivery of topiramate nanoemulsion: Pharmacodynamic, pharmacokinetic and brain uptake studies.


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
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

119486

Informations 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.

Auteurs

Ravish J Patel (RJ)

Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, CHARUSAT Campus, Changa-388 421, Anand, Gujarat, India. Electronic address: ravishpatel.ph@charusat.ac.in.

Rajesh H Parikh (RH)

Graduate School of Pharmacy, Gujarat Technological University, Ahmedabad, Gujarat, India.

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Classifications MeSH