Abstract
Objective: To develop and evaluate the mucoadhesive microsphere using combinations of natural polymers chitosan and xanthan gum for sustained release.
 Methods: In the present work mucoadhesive microspheres were prepared by using natural polymers like chitosan and xanthan gum by using the emulsion chemical cross-linking method. Chemical cross-linking was done by using glutaraldehyde. The 22 factorial design was employed to show the effect of cross-linking agent and processing factor-like stirring and speed. Prepared microspheres were evaluated for their particle size, surface morphology, drug entrapment efficiency, in vitro drug release, swelling index, and mucoadhesive strength.
 Results: The size of microspheres of factorial batches were in the range of 26-46 µm. The swelling index was showed in the range of 1.51-1.66 percentage. The equation of multiple regression revealed that there was significant interaction among factors. The glutaraldehyde concentration had a positive effect on % entrapment efficiency, % cumulative drug release and % mucoadhesion. Stirring speed showed a negative impact on % entrapment efficiency, % cumulative drug release and % mucoadhesion. The interactive effect of glutaraldehyde concentration and the stirring speed was found to be positive for % entrapment efficiency and % cumulative drug release. In vitro drug release study of optimized formulation F2 show 96 % of drug release with 6 h indicating sustained release behavior with diffusion mechanism. The SEM image of the optimized batch was spherical with a porous surface.
 Conclusion: The results obtained in this research work indicated that a promising potential of chitosan and xanthan gum combination for the preparation of the mucoadhesive microsphere of Racecadotril.
Highlights
The concept of multiple unit dosage forms was initially introduced in the early nineteen-fifties
The IR spectra did not show any significant difference from those obtained for their physical mixture. These results indicated that the above polymer can be used without any interaction for the preparation of the Mucoadhesive Microsphere of Racecadotril
Differential scanning calorimetry analysis (DSC) DSC thermograph of a given sample of Racecadotril is shown in fig
Summary
The concept of multiple unit dosage forms was initially introduced in the early nineteen-fifties. Recent trends showed that the multiparticulate drug delivery system is suitable for achieving the controlled release or prolong release formulations with no risks of dose dumping. Multiparticulate drug delivery system provides incredible opportunities for designing controlled release formulations [1,2]. Mucoadhesion is the topic of current interest in the design of the drug delivery system to prolong the residence time of the dosage form. The mucoadhesive system adheres to the mucus This adhesion is a result of electrostatic and H-bond formation at the mucus-polymer boundary. Racecadotril is rapidly absorbed from the gastrointestinal tract This drug has a repetitive dose schedule (100 to 300 mg thrice daily up to 7 d in continue treatment), short biological half-life (3 h) and reduced bioavailability (30–40 %)
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