Rectal Suppository of Mucoadhesive Microspheres of Alverine Citrate for İrritable Bowel Disease: In vitro Evaluation

Abstract

The aim of present investigation was to develop chitosan based mucoadhesive microspheres of alverine citrate (ALV) for rectal delivery. Mucoadhesive microspheres of alverine citrate were prepared by simple emulsification crosslinking technique and evaluated for surface morphology, particle size, equilibrium swelling degree, drug content, in vitro bioadhesion and in vitro drug release. The suppositories of optimized batch of microspheres (AM5) were prepared by fusion method using cocoa butter, polyethylene glycol (PEG) 2000, PEG 4000 alone or in combinations with different ratios and evaluated for weight variation, hardness, drug content uniformity, liquefaction time, micro-melting range, in vitrodissolution and compatibility study by Attenuated total reflectance- Fourier transform infrared spectroscopy (ATR-FTIR). Chitosan based mucoadhesive microspheres of all batches of ALV except AM3 and AM4 showed spherical shape and particle size in the range of 76.56 to 294.32µm. All the formulations showed drug encapsulation efficiency in the range of 43.91 to 98.36% and bioadhesion in the range of 58.25 to 82.65%. AM5 batch showed 94.65% drug release at the end of 10h. Formulations of solid suppositories showed all the physical parameters within prescribed pharmacopoeial standard limits. Drug content of all the batches of suppositories was found to be in the range of 70.94 to 91.65%. All the batches of suppositories retarded the release of drug at the end of 10h. Suppository batch E showed 86.33% drug release at the end of 10h. Developed rectal formulation of ALV could be able to relieve the symptoms of irritable bowel disease and may overcome the disadvantages of oral delivery.