Chitosan Loaded Mucoadhesive Microspheres of Gliclazide - Journal

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A Senthil et al./ Chitosan Loaded Mucoadhesive Microspheres of Gliclazide: In vtro and In vivo Evaluation Table 1: Preliminary Trial Batches of Gliclazide Mucoadhesive Microspheres Loaded Chitosan Batch Vol. of Cross- % Drug Sphericity of code Glutaraldehyde linking Mucoadhesion Entrapment Microsphere (mL) time(hr) after 1 hr. Efficiency (%) F1 10 1 84 40 Very Irregular F2 10 2 82 42 F3 10 3 79 44 F4 10 4 77 46 F5 20 1 86 52 Slightly Irregular F6 20 2 78 55 F7 20 3 72 58 F8 20 4 68 60 F9 40 1 78 57 Spherical free flowing F10 40 2 69 59 F11 40 3 64 60 F12 40 4 60 62 F13 60 1 78 60 F14 60 2 68 62 F15 60 3 64 64 F16 60 4 58 64 F17 70 1 59 64 F18 70 2 52 69 F19 70 3 45 70 F20 70 4 39 71 Note: All batches were prepared by polymer-to-drug ratio of 3:1 at 1000 rpm stirring speed Table 2: Formulations of Chitosan Loaded Gliclazide Mucoadhesive Microspheres by 3 2 Full Factorial Design Layout Variable levels in % Drug Swelling Particle Batch coded from Mucoadhesion Entrapment Index Size Code X 1 X 2 After1 hours Efficiency (%) A1 -1 -1 52 54.25 0.888 60.6 A2 -1 0 46 52.68 0.824 58.2 A3 -1 1 43 49.12 0.812 50.2 A4 0 -1 78 72.00 1.182 67.1 A5 0 0 69 70.84 1.123 64.0 A6 0 1 62 66.96 1.082 60.8 A7 1 -1 80 77.12 1.412 98.0 A8 1 0 73 73.54 1.298 89.8 A9 1 1 67 70.67 1.242 74.4 Note: All batches were prepared using 60 mL of glutaraldehyde and cross-linking time of 1 hours Translation of coded levels in actual units Variables level Low (-1) Medium (0) High (+1) Polymer-to-drug ratio (X 1 ) 1:1 3:1 6:1 Stirring speed (X 2 ) rpm 500 1000 1500 166 RJPS, Jul - Sep, 2011/ Vol 1/ Issue 2
polymer-to-drug ratio respectively, have shown good correlation coefficient 0.9984. Results of the equation indicate that the effect of (X ) polymer-to-drug ratio is more 1 significant than (X ) stirring speed. However stirring speed has 2 a negative effect on drug entrapment efficiency, hence the stirring speed increased, the particle size decreased, and the drug entrapment efficiency has also decreased. The particle size of the mucoadhesive microspheres of chitosan varied from 50 to 98 µm and has shown good correlation coefficient 0.9878. However stirring speed has a negative effect on particle size, thus the stirring speed increased, the particle sizes decreased. 2 Y= 67.1 + 4.69 X1 - 4.47 X2 - 0.98 X2 - 0.98 X1 X2 Factorial equation for percentage mucoadhesion and swelling index The in vitro wash-off test for percentage mucoadhesion of chitosan loaded mucoadhesive microspheres after 1 hour varied from 43% to 52%, 62% to 78% and 67% to 80% at lower, medium and higher levels of polymer-to-drug ratio and has shown good correlation coefficient 0.9803. However stirring speed has a negative effect on percentage mucoadhesion. As the polymer-to-drug ratio increases, the percentage mucoadhesion also increases; because more amounts of polymer results in higher amount of free-COOH groups, which are responsible for binding with sialic acid groups in mucus membrane and thus results in increase in mucoadhesive properties of microspheres. In vitro mucoadhesive test has shown that gliclazide mucoadhesive microspheres adhered more strongly to gastric mucous layer and would retain in gastrointestinal tract for an extended period of time were shown in (Fig.1). 2 Y= 77.81 + 15.78 X1 - 6.91 X2 - 9.98 X2 - 2.1X1 X2 A Senthil et al./ Chitosan Loaded Mucoadhesive Microspheres of Gliclazide: In vtro and In vivo Evaluation The microspheres (100) were suspended in 5 mL of simulated gastric fluid USP (pH 1.2). The particle size would be monitored by microscopy technique every 1 hour using an optical microscope. The increase in particle size of the microspheres would be noted up to 8 hours. The swelling index of chitosan varied from 0.812 to 1.412. Surface graphs showing effect of variables on % mucoadhesion, drug entrapment efficiency, swelling index and particle size for optimized batch were shown in (Fig. 2). Chitosan could be covalently cross-linked with glutaraldehyde through its amino groups. The aldehyde groups of the glutaraldehyde formed covalent imine bonds with the amino groups of chitosan, due to the resonance established with the adjacent double ethylenic bonds via a Schiff reaction. It is reflects that polymeric chains during cross-linking procedure, the extent of the swelling index depends on the cross-linking. Therefore, 167 Fig. 1: In vitro Wash-Off Test Carried out on Gliclazide Loaded Chitosan Mucoadhesive Microspheres (batch A4), using Rat Stomach Figure 2: Surface Graphs Showing Effect of Variables on (1) % Mucoadhesion (2) Drug Entrapment Efficiency (3) Swelling Index (4) Particle Size for Optimized Batch (A4). 1 2 3 4 the denser the cross-linking bridges between the chitosan molecules, the more packed is the structure. Such structure can be characterized by lower and slower penetration of the solvent through the chain structure of the polymer, suggesting that the swelling ratio and hence the release characteristics of the microspheres can be controlled by varying the content of the cross-linking agent used during the manufacturing process. Since glutaraldehyde is responsible for the formation of cross-links, increasing the amount of glutaraldehyde and RJPS, Jul - Sep, 2011/ Vol 1/ Issue 2
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