Formulation and in vitro evaluation of pH sensitive oil entrapped polymeric blended gellan gum buoyant beads of clarithromycin

ABSTRACT

A gastroretentive pH sensitive system has been a frontier approach to release the drug in controlled manner in stomach and duodenum. The aim of this study was to develop buoyant beads of gellan based, wherein, the oil was entrapped, blended with hydroxypropyl methyl cellulose or carbopol 934 in order to evaluate its potential for targeted sustained delivery of clarithromycin in the gastric region. Buoyant beads of gellan was developed by inotropic gelation technique using calcium carbonate as gas forming agent and the drug polymer dispersion was emulsified with mineral oil. The oil was entrapped and blended with hydroxypropyl methyl cellulose or carbopol 934. The developed beads were evaluated in terms of diameter,% floating, encapsulation efficiency, In vitro drug release, in vivo gastric residence efficacy and clarithromycine concentration in the mucosa of the experimental animal model. The scanning electron microscope photograph indicated that the prepared beads were spherical in shape and buoyancy, encapsulation efficiency and drug content obtained from all batches were satisfactory. Particle size and percentage buoyancy of the gel beads increased by raising the concentration of calcium carbonate. The formulation exhibited sustained release profile and was best fitted in the Peppas model with n < 0.45. Subsequent coating of microbeads exhibited zero-order sustained pattern of the drug release up to 8 hrs. Batch B4 showed comparatively better residence and the drug concentration in the gastric mucosa of the treated animals. The result provides evidence that the prepared optimized formulation may be used effectively for pH sensitive gastric targeted antibiotic such as clarithromycin