Transferosomes for Trans-Nasal Brain Delivery of Clonazepam Preparation Optimization Ex Vivo Cytotoxicity and Pharmacodynamic Study
Journal Title: Open Access Journal of Pharmaceutical Research - Year 2017, Vol 1, Issue 2
Abstract
Clonazepam (CZ) is a benzodiazepine derivative that is used mainly in the treatment of status epilepticus (SE). Intranasal (IN) administration of nano-carrier systems generally have the ability to deliver the drug to the brain through olfactory and trigeminal nerves pathways circumventing the blood brain barrier (BBB). The aim of the present work was to enhance intranasal (IN) brain delivery of clonazepam in an attempt to treat status epileticus (SE). In order to achieve this goal, clonazepam transferosomes (TF) were prepared via thin film hydration technique (TFH) adopting 22 X 31 full factorial design (FFD). The twelve formulae were evaluated in terms of entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and in-vitro release. TF1 prepared using sodium deoxycholate (SDC) as edge activator (EA), lipid to edge activator molar ratio of 10:1 and 10 mg as initial drug amount showed the highest desirability value of 0.833. The optimized formula showed minor changes to sheep nasal mucosa upon ex-vivo cytotoxicity study and significant delay in the onset of pentylenetetrazole (PTZ) induced seizures. The declared results reveal the ability of the developed TF to be a strong potential candidate for the emergency treatment of SE.
Authors and Affiliations
Nour SA*, Abdelmalak NS and Naguib MJ
Keywords
Related Articles
- EP ID EP745753
- DOI 10.23880/oajpr-16000107
- Views 30
- Downloads 0
Mechanistic Insights of Rutin against Metabolic Disorders
Rutin, a quercetin glycoside comes under the class flavonol. The aglycone part of rutin is known as quercetin. It is found in numerous fruits and plants, especially apricots, buckwheat, cherries, grapefruit, grapes, ora...
Review on Novel Monoamine Oxidase Inhibitors: A Clinician’s Guide
The purpose of this review is to provide information on the mechanisms of action, pharmacokinetics, therapeutic effectiveness, safety, and tolerability of four novel antidepressants: pirlindole, safinamide, selegiline,...
Development of an Antihypertensive Loaded Solid Lipid Nanoparticle
Solid lipid nanoparticles were prepared by using the solvent evaporation method. The prepared solid lipid nanoparticles of felodipine from different batches were weighed accurately and filled into appropriate-sized caps...
Sustained Release Multiple Unit Dosage Form for the Oral Day Delivery of Dexketoprofen Trometamol
The aim of this study was to prepare sustained release multiple unit dosage form (MUDF) for the oral day delivery of the frequently administered and the highly water soluble drug, dexketoprofen trometamol (DT). The drug...
Carbohydrates Test and In Vitro Inhibitory Activities of AlphaGlucosidase and Alpha-Amylase of Stem Bark Extracts of Musanga Cecropioides
Elevated postprandial hyperglycemia is one of the risk factors linked to diabetes. Decreasing postprandial hyperglycemia is possible by inhibiting certain carbohydrate hydrolyzing enzymes like α-amylase and α-glucosidase...