Abstract
BackgroundThe current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ). The study objective was to improve the oral bioavailability along with prolongation of its duration of action for a better glycaemic control. Ionic gelation technique was employed in formulating the dosage form. Optimization of the batches was carried out by response surface methodology using 32 full factorial designs. The microsphere prepared was characterized for several parameters along with its in vitro release study. The gastrointestinal transit of the optimized batch of prepared microspheres after oral administration was studied in rabbits by using the gamma scintigraphy technique utilizing 99mTc as the labelling agent in the presence of stannous chloride. Also, the optimized batch was studied for its pharmacokinetic parameters. Moreover, the antidiabetic efficacy of the prepared microsphere was evaluated in rats by using the streptozotocin (STZ)-induced diabetic model.ResultsThe factorial design experiment resulted in an optimum formulation coded as F8. The compatible nature of the drug and excipient was revealed from FTIR, DSC and IST studies. The scanning electron micrographs also showed the occurrence of spherical microspheres having a smooth surface. The in vitro release study provided an evidence of an initial burst effect that was followed by a prolong release phase. The pharmacokinetic parameters justified the ability of the prepared dosage form in sustaining the drug release with a 2.7-fold enhancement in drug bioavailability. The images obtained during the gamma scintigraphy study suggested the gastro-retentive nature of the dosage form with the gastro-retentive ability for more than 4 h. Also, the pharmacodynamics study carried out in diabetic rat model confirmed about the better efficacy of the dosage form in lowering the elevated blood glucose level.ConclusionThe overall study data provide valuable information about the potential of this banana starch in formulation of a mucoadhesive dosage form that can be used for enhancement of bioavailability of drug-like gliclazide which in turn can provide a beneficial effect in the management of diabetes.
Highlights
The current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ)
Nine batches of gliclazide-loaded mucoadhesive microsphere were prepared to vary the concentration of the MSB-Starch and Na-alginate and varying the concentration of cross-linking agent CaCl2
9 different formulations were prepared by altering the ratio of polymer and cross-linking agents and the results obtained by evaluation of the prepared formulation were added to the software in order to achieve the results for model significance
Summary
The current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ). There is always a major challenge for developing an orally active sustained release dosage form. The shorter residence time of this delivery system, at the absorption site, is the main limitation, which decreases the utility This major limitation can only be overcome if an approach for establishing a firm contact of the drug delivery system with the absorbing membrane is carried out. This can be achieved by incorporating bioadhesion characteristics to the micro-particles, thereby developing delivery systems referred to as "bioadhesive micro particles" [3]. The concept of bioadhesion combines the advantage such as enhancement of drug continuance mostly at the absorption site, and it has been applied to various formulations to target different parts in the GI tract
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