Background: Buspirone Hydrochloride is an anxiolytic agent and serotonin receptor agonist
belonging to azaspirodecanedione class of compounds used in the treatment of anxiety disorders.
It has short half-life (2-3h) and low oral bioavailability (4%) due to extensive first pass metabolism.
Objective: The nasal mucosa has several advantages viz., large surface area, porous endothelial membrane,
high blood flow, avoidance of first-pass metabolism and ready accessibility that lead to faster
and higher drug absorption. Keeping these facts in mind, the objective of the present study was to develop
Buspirone hydrochloride loaded niosomal in-situ nasal gel.
Method: Buspirone hydrochloride niosomal in situ nasal gel was formulated, optimized and evaluated
with the objective to deliver drug to the brain via intranasal route. Niosomes were prepared by
thin film evaporation method and optimized using32 factorial design. Niosomes were characterized for
particle size, zeta potential, entrapment efficiency and in vitro drug release. Buspirone hydrochloride
loaded niosomes were further incorporated into Carbopol 934P and HPMC K4M liquid gelling system
for the formation of in situ gel. The resultant solution was assessed for various parameters, viz., gelling
time, gelling capacity, viscosity at pH 5 and pH 6.
Result: The vesicle size of all niosomal suspension batches ranges between 168.3 -310.5 nm. The
vesicle size of optimized niosomal suspension F5 batch is 181.9±0.36nm. For F5 batch, the value of
zeta potential was found to be -15.4 mV; this specifies that prepared niosomes have sufficient surface
charge to prevent aggregation of the vesicles. % entrapment efficiency for all batches was found in the
range 72.44±0.18% to 87.7±0.66%. The cumulative percent release of niosomal suspension ranges
from 66.34±0.39 to 84.26±0.26%. Ex vivo permeation of Buspirone hydrochloride through the sheep
nasal mucosa showed that 83.49% w/w drug permeated after 8 h. The SEM and Zeta potential studies
showed the formation of stable vesicles.
Conclusion: Thus, the application of niosomes proved the potential for intranasal delivery of Buspirone
hydrochloride over the conventional gel formulations. Overall intranasal drug delivery for Buspirone
hydrochloride has been successfully developed.