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Updated: May 5, 2026

Novel Methods for Intranasal Administration Under Inhalation Anesthesia to Evaluate Nose-to-Brain Drug Delivery
Published on: November 14, 2018
Chitosan and cyclodextrin in intranasal microemulsion for improved brain buspirone hydrochloride pharmacokinetics in
Hamza Bshara1, Rihab Osman, Samar Mansour
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African Organization Unity Street, P.O. Box 11566, Cairo, Egypt.
Abstract:
The aim of this study was to develop buspirone hydrochloride microemulsion formulations for intranasal administration to improve the drug bioavailability and provide high drug brain levels. For the purpose, chitosan aspartate, and hydroxypropyl-β-cyclodextrin were incorporated in the microemulsions. The prepared formulations were characterized. Biological investigations including pharmacokinetic studies, brain drug targeting efficiency determinations and histopathological examinations were performed on rats. The results showed that safe and stable mucoadhesive microemulsion suitable for nasal administration were successfully prepared. Ex vivo drug permeation revealed high drug permeation from microemulsions. Absolute bioavailability after intranasal administration of buspirone mucoadhesive microemulsion increased significantly and plasma concentration peaked at 15 min. The AUC0-360(brain) was 3 times that obtained after intravenous administration. A high brain targeting efficiency (86.6%) and a direct nose to brain transport (88%) confirmed the direct nose to brain transport of buspirone following nasal administration of the microemulsions.
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