DEVELOPMENT CHARACTERIZATION AND EVALUTION OF NASAL IN SITU GEL OF TRAZODONE HCl
M. Himabindu and Kopparam Manjunath*
ABSTRACT
In situ hydrogels are instilled as drops in the nasal and undergoes a
solution to gel transition, improving nasal bioavailability by increasing
the duration of contact, thereby reducing the frequency of
administration. In this study, a nasal drug delivery system was
developed using two different gelling agents with different
mechanisms (pH and ion method) for in situ gelation of Trazodone
HCl, an anti-depressant drug. In pH triggered method Carbopol 934
was used as a pH triggered polymer. Different formulations were
prepared by varying the concentrations of Carbopol 934 alone and in
combination with HPMC K 100. In case of ion activated method,
Trazodone HCl in-situ nasal gel (0.1% w/w) were prepared at
concentration of Gellan Gum (0.3, 0.4, 0.5 ,0.6% w/v) and HPMC E15 M (0.1, 0.15% w/v).
The formulations were evaluated for hydrogel formation, pH, viscosity, in vitro release, drug
content. The formulation of (1:1) carbopol 934 with HPMC K100 and gellan gum (0.4%)
with HPMC E15 (0.15%) was tested for stability studies. Release kinetics followed zero
order (non fickian) model. FTIR study revealed that there was no interaction between drug
and polymer. pH of all the formulations were found to be in the range of 3.84-4.29 (pH
method) and 4.88-6.39 (ion method) and the drug content for all the prepared formulations
was found to be in the range of 84-95% (in pH) and 85-96% (ion activated).The results of in
vitro drug release indicated that the optimized formulation F7 and F12 is the most successful
formulation of the study, exhibited a sustained drug release of 55.48% – 87.33% (in pH
method) and 68.41% – 88.79% (ion method) in 8 hours with viscosity 4.68 (in pH method)
and 114.3 (ion method).
Keywords: Nasal in situ gel, Trazodone HCl, pH method, ion dependent method.
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