Intranasal delivery of topiramate nanoemulsion: Pharmacodynamic, pharmacokinetic and brain uptake studies
[Display omitted] •Epilepsy is characterized by frequent and unprovoked seizures in the brain.•Thermodynamically stable topiramate nanoemulsion was assessed for brain uptake.•Higher brain uptake was observed post intranasal delivery of TPMNE.•The intranasal delivery of topiramate nanoemulsion improv...
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Veröffentlicht in: | International journal of pharmaceutics 2020-07, Vol.585, p.119486, Article 119486 |
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Format: | Artikel |
Sprache: | eng |
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•Epilepsy is characterized by frequent and unprovoked seizures in the brain.•Thermodynamically stable topiramate nanoemulsion was assessed for brain uptake.•Higher brain uptake was observed post intranasal delivery of TPMNE.•The intranasal delivery of topiramate nanoemulsion improves brain uptake.
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 |
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ISSN: | 0378-5173 1873-3476 |
DOI: | 10.1016/j.ijpharm.2020.119486 |