Chitosan Loaded Mucoadhesive Microspheres of Gliclazide - Journal

A Senthil et al./ Chitosan Loaded Mucoadhesive Microspheres of Gliclazide: In vtro and In vivo Evaluation
Fig.3: Counter Plot showing the Effect of Polymer-to-
Drug Ratio (X1) and Stirring Speed (X2) on: %
Mucoadhesion (a), Swelling Index (b), Drug Entrapment
Efficiency (c), Particle Size (d) for Optimized Batch (A4).
a b
c d
Fig. 4: Percentage Reduction in Blood Glucose Levels
following Oral Administration of Pure Drug and Formulation
in Normal Rats (n = 5)
the same dose. Gliclazide pure drug was administered, a rapid
reduction of 42.83% was observed within 2 hours after oral
administration. Blood glucose levels were recovered rapidly to
the normal level within 8 hours. In the chitosan loaded
gliclazide mucoadhesive microspheres, the reduction in blood
glucose levels was slow and reached maximum reductions
within 4 hours after oral administration were shown in (Fig. 4).
This reduction in blood glucose levels was sustained over a
longer periods of time 10 hours. Kahn and Shechter have
suggested that a 25% reduction in blood glucose level is
34
considered a significant hypoglycemic effect . 25% of
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hypoglycemic effect was maintained for a period of 0.5 to 2
hours period after oral administration of pure gliclazide. In
the case of gliclazide mucoadhesive microspheres shows
significant hypoglycemic effects was maintained for a period
of 1 to 9 hours. The sustained hypoglycemic effect observed
over long period of time because of the mucoadhesive
microspheres is due to slow release of drug and absorption of
gliclazide over longer periods of time. Gliclazide sustained
release formulation is significantly more effective than the
immediate release formulation of gliclazide in reducing
fasting plasma glucose levels and side effects as per Berelowitz
35
et al . The optimized batch A4 was studied its potential and
associated to control blood glucose level in animal. In this
study sustained release mucoadhesive microspheres of
gliclazide exhibited significant important in diabetic
parameters like glucose as compared to immediate release
formulation of sustained drug gliclazide. It may be the other
polysaccharides such as starch and other additive also contain
the precursors of glucose in the formulation of oral dosage
forms administrated available in market. The result reflects
that mucoadhesive microspheres were sustain regimen
maintain the vivo significant effect in animal models were
shown in (Fig. 4).
Stability studies revealed that, there was a reduction in
entrapment efficiency after storage for one month at 4±1°C,
25±2°C 25±2°C 60±5% RH and 37±2°C have shown
maximum entrapment followed by the storage at 25±2°C at
60±5% RH and 37±2°C at 65 ± 5% RH conditions. A4
batch stored at 4±1°C has shown 91.12 % drug release, at
25±2°C with 60±5% RH has shown 95.32% and at 37±2°C
with 65±5% RH has shown 98.76%, and the percentage of
drug entrapment efficiency at 4±1°C, 25±°C with 60±5%
RH and 37±2°C with 65±5% RH for one month was found
to be 72%, 72% and 69%.
The IR spectra of the pure drug gliclazide as well as the
combination spectra of the drug and polymers. In all the
combinations the wave numbers related to aliphatic
secondary amine, carbonyl, sulphur-oxy groups were nearly
same, which indicates no interaction between gliclazide and
polymers.
CONCLUSION
2
The results of a 3 full factorial design revealed that the
polymer-to-drug ratio and stirring speed significantly affected
the dependent variables percentage mucoadhesion, drug
entrapment efficiency, particle size and swelling index. As the
concentration of glutaraldehyde increases, the
mucoadhesiveness decreases and there was no significant
effect in time. Stirring speed has negetive effect on drug
RJPS, Jul - Sep, 2011/ Vol 1/ Issue 2