Objectives: The goal of the study was to develop, optimize and
in vitro-
ex vivo
investigation of Brimonidine tartrate nanosuspension incorporated
in situ gel formulation
to differentiate with marketed (formulation) eye drops for the efficient treatment of
glaucoma. Materials and Methods: Nanosuspensions were formulated by solvent
evaporation method using probe sonication technique. The effect of the independent
variables Tween 80 and Pluronic F68 concentration on Nanosuspension properties were
investigated by performing 32 factorial design of experiment. Nanosuspensions were
characterized by measuring particle diameter and zeta potential, surface morphology,
drug entrapment efficiency and then nanosuspensions were incorporated in to
in situ gel
base for
in vitro release and
ex-vivo corneal permeability studies and were differentiated
with marketed product. Results and Discussion: The most excellent nanosuspension
formulation system selected via the Design Expert 12 software program was F7 which
contains 0.5% of Tween 80 and 3 % of Pluronic F68. An optimized nanosuspension
formulation F7 showed an average particle diameter of 157.4±0.95 nm with PDI of
0.379 and a zeta potential of -19.1 mV. It had an average entrapment efficiency of
85.95±1.40%. It also showed 98.36±0.58% of drug being released
in vitro when
incorporated in to
in situ gel base over 24 hr. F7 showed significantly greater drug
permeation in comparison to the marketed eye drop formulation in
ex vivo transcorneal
permeability studies and was able of retaining its stability for 90 days. Conclusion: The
developed nanosuspension incorporated
in situ gel base formulation could be utilized as
potential delivery system for long time management of glaucoma with once daily dose.