Mucoadhesive Nanoemulsion of Safranal for the Treatment of Epilepsy

Safranal a major bioactive constituent of saffron, Crocus sativus L., of the Iridaceae family has demonstrated promising anti-convulsant effects in preclinical studies [1,2]. With the objective to accomplish the rapid delivery of safranal to the brain nasally to treat convulsive disorders, safranal nanoemulsions (SNE) were prepared by an aqueous titration method. The developed formulations were characterized for globule size, drug content, percentage transmittance and pH. The optimized SNE containing 99.83% safranal had a globule size of 45±0.15nm, percent transmittance of 97.12 and pH of 6.6. The chitosan coated mucoadhesive nanoemulsion (SMNE) had a zeta potential of 31.7±0.1 mV. Gamma scintigraphic images revealed significantly higher brain/blood uptake ratio for SMNE following intranasal administration (1) (0.846) compared to intranasal safranal (2) (0.252, used as such) and SMNE following intravenous administration (0.532). The results indicated that nose to brain delivery of SMNE bypasses the blood-brain barrier resulting in effective brain targeting of safranal. Studies conclusively demonstrated rapid and larger extent of transport of safranal by intranasal SMNE compared to intranasal safranal and intravenous SMNE into the rabbit brain. Thus intranasal administration of SMNE might play a promising role in the treatment of epilepsy.

References: [1] Hosseinzadeh H, Sadeghnia HR (2007) Phytomed 14: 256–262. [2] Hosseinzadeh H, Younesi HM (2002) BMC Pharmacol 2: 1–8.