Enhanced Brain Uptake and Behaviour Study of Buspirone Loaded in situ Nanoemulsion Gel

Kamalesh Tripathi and Niranjan K. Manna

Background and Objective: Nose-to-brain delivery is the most fascinating application, bypassing the blood-brain barrier and directly targeting the brain receptor. Buspirone is indicated for the treatment of generalized anxiety disorder, relieve symptoms of anxiety and unipolar depression. This drug exhibit low bioavailability (approximately 5%), extensive first-pass metabolism and non-targeted delivery results in numerous side effects. The reported experimental study was conducted to explore the potential of buspirone-loaded in situ nanoemulsion gel (BNG) to the brain delivery via nasal route. Materials and Methods: Effect of single daily nasal administration was compared in Wistar rats for locomotor activity, marble burying and elevated plus maze model. Thereafter, buspirone concentration in brain tissue was determined by multiple time point pharmacokinetic study. The analysis of the drug was carried out on the HPLC system. Results: A statistically significant effect of Buspirone-loaded Nanoemulsion (BNE) and BNG as compared to the nasal solution was observed in the present investigation. Biodistribution of BNE, BNG, Buspirone Plain Solution (BHP) and Buspirone Solution (BHS) in the brain and blood of swiss albino rats following Intranasal (IN) and Intravenous (IV) administration was examined. The brain blood uptake ratio of 0.889, 2.398, 2.779 and 0.102 for BHP (intranasal), BNE (intranasal), BNG (intranasal) and BHS (IV), respectively at T_max are indicative of direct nose to brain transport bypassing the blood-brain barrier. Higher direct transport percentage (93.00%) and Drug Transport Efficiency (DTE>1) confirm the direct pathway from the nose to the brain. Conclusion: Reports imply that the pharmacokinetic and pharmacodynamics study used in this investigation is well suited for optimization of spatial and temporal targeting. The finding of reported results reveals, a rapid and larger extent of transport of BNG and BNE, which confirms that in situ nanoemulsion gel containing buspirone could be used as an intranasal formulation for targeted brain delivery.

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