Diazepam is an anticonvulsant effective in the prevention and treatment of epileptic seizure emergencies. It is presently administered either intravenously or rectally in emergency situations; however, neither of these delivery routes is desirable. Since the nose is one of the most permeable and highly vascularized sites for drug administration, ensuring rapid absorption and onset of therapeutic action, nasal administration of diazepam is a potential alternative to intravenous injections and rectal administration in treatment of acute epileptic seizures.
Diazepam has low water solubility (0.05 mg/ml), so aqueous nasal diazepam is not feasible. However, in other solvents in which diazepam has higher solubility, the activity of diazepam, and hence its tendency to cross nasal mucosa, is not enhanced. We have found that diazepam can be formulated, in mixed water/glycofurol cosolvents, to remain in a high activity, supersaturated state for many hours under proper mixing conditions, and we expect to see enhanced nasal permeation with such preparation. Pursuing this idea, a microfluidic point-of-administration system, based on chaotic advection, is being developed.